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重酒石酸卡巴拉汀
Tier B · 提前布局Rivastigmine Tartrate
诺华制药
原研
1998
首批上市
-
到期年（公开口径）
$1.09B ▲
峰值销售
化学药
类型
靶点：AChE、BChE
商品名：Exelon、Exelon MR、Exelon TDS、Rivastach、Prometax、艾斯能
适应症（已批准）：阿尔茨海默病、痴呆、帕金森病
各地区研发/上市状态
美国
临床二期
2009-11-01
欧盟
批准上市
1998-05-11
中国
批准上市
2018-05-23
日本
批准上市
2011-04-22
合成路线与中间体27 routes
原研路线 × 1优化路线（非专利）× 26工艺路线 × 0
路线按「原研路线 → 优化路线 / 工艺路线（非专利）」排序。每条路线附本站自绘的路线流程图（中间体 → 原料药）与中间体表（编号 / CAS / 英文名），可直接用于供应商开发与询价。流程图由本站依据已授权的结构化数据自行渲染，未使用任何第三方路线图。
原研Route 1步骤 2 · 总收率 /
RIVAT-001105601-04-5RIVAT-00288-10-8RIVAT-003105601-20-5API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| RIVAT-001 | 105601-04-5 | 3-(1-(dimethylamino)ethyl)phenol |
| RIVAT-002 | 88-10-8 | diethylcarbamic chloride |
| RIVAT-003 | 105601-20-5 | 3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
优化Route 2步骤 4 · 总收率 /
RIVAT-0041243322-19-1RIVAT-005139306-10-8RIVAT-006139306-10-8RIVAT-00742252-34-6RIVAT-00832315-10-9API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| RIVAT-004 | 1243322-19-1 | (S)-1-(3-(methoxymethoxy)phenyl)ethanamine |
| RIVAT-005 | 139306-10-8 | (S)-3-(1-(dimethylamino)ethyl)phenol |
| RIVAT-006 | 139306-10-8 | (S)-3-(1-(dimethylamino)ethyl)phenol |
| RIVAT-007 | 42252-34-6 | ethyl(methyl)carbamic chloride |
| RIVAT-008 | 32315-10-9 | bis(trichloromethyl) carbonate |
优化Route 3步骤 5 · 总收率 4.6 kg
RIVAT-00742252-34-6RIVAT-009121-71-1RIVAT-010—RIVAT-0111233378-72-7RIVAT-0121233378-78-3RIVAT-013139306-10-8API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| RIVAT-007 | 42252-34-6 | ethyl(methyl)carbamic chloride |
| RIVAT-009 | 121-71-1 | 1-(3-hydroxyphenyl)ethan-1-one |
| RIVAT-010 | - | (R)-3-(1-hydroxyethyl)phenol |
| RIVAT-011 | 1233378-72-7 | (R)-3-(1-((methylsulfonyl)oxy)ethyl)phenyl methanesulfonate |
| RIVAT-012 | 1233378-78-3 | (S)-3-(1-(dimethylamino)ethyl)phenyl methanesulfonate |
| RIVAT-013 | 139306-10-8 | (S)-3-(1-(dimethylamino)ethyl)phenol |
优化Route 4步骤 4 · 总收率 7.43 g
RIVAT-00742252-34-6RIVAT-009121-71-1RIVAT-014855300-09-3RIVAT-0151257519-35-9RIVAT-016—API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| RIVAT-007 | 42252-34-6 | ethyl(methyl)carbamic chloride |
| RIVAT-009 | 121-71-1 | 1-(3-hydroxyphenyl)ethan-1-one |
| RIVAT-014 | 855300-09-3 | 3-acetylphenyl ethyl(methyl)carbamate |
| RIVAT-015 | 1257519-35-9 | (S)-3-(1-hydroxyethyl)phenyl ethyl(methyl)carbamate |
| RIVAT-016 | - | (R)-3-(1-bromoethyl)phenyl ethyl(methyl)carbamate |
优化Route 5步骤 2 · 总收率 173.00 mg
RIVAT-01710401-11-3RIVAT-0181643442-41-4API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| RIVAT-017 | 10401-11-3 | 3-ethynylphenol |
| RIVAT-018 | 1643442-41-4 | 3-ethynylphenyl ethyl(methyl)carbamate |
优化Route 6步骤 5 · 总收率 /
(I)145089-1-a121-71-1(II)145089-1-a63720-38-7(III)145089-1-a105601-04-5(IV)145089-1-a42252-34-6(V)145089-1-a105601-20-5(VI)145089-1-a—(VII)145089-1-a530-62-1(VIII)145089-1-a624-78-2(IX)145089-1-a123441-03-2API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-1-a | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (II)145089-1-a | 63720-38-7 | 3-(1-Aminoethyl)phenol |
| (III)145089-1-a | 105601-04-5 | 3-[1-(Dimethylamino)ethyl]phenol |
| (IV)145089-1-a | 42252-34-6 | N-Ethyl-N-methylcarbamic chloride |
| (V)145089-1-a | 105601-20-5 | N-Ethyl-N-methylcarbamic acid 3-[1-(N,N-dimethylamino)ethyl]phenyl ester |
| (VI)145089-1-a | - | Formic acid N-methylmethanamine |
| (VII)145089-1-a | 530-62-1 | 1-[(1H-Imidazol-1-yl)carbonyl]1H-imidazole |
| (VIII)145089-1-a | 624-78-2 | N-Ethyl-N-methylamine |
| (IX)145089-1-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
优化Route 7步骤 8 · 总收率 /
(I)145089-2-a121-71-1(II)145089-2-a,(II)145089-2-e586-37-8(III)145089-2-a122806-25-1(IV)145089-2-a62409-13-6(V)145089-2-a198756-81-9(VI)145089-2-a,(VI)145089-2-c889443-69-0(VIIa)145089-2-a139306-10-8(VIIb)145089-2-a—(VIIIa)145089-2-a42252-34-6(VIIIb)145089-2-a928032-01-3(IX)145089-2-a123441-03-2(X)145089-2-a—(XI)145089-2-a1071141-86-0(XII)145089-2-a,(XII)145089-2-e120523-12-8(XIII)145089-2-a1647103-52-3(XIV)145089-2-a124-40-3(XV)145089-2-a1810713-46-2(XVI)145089-2-a,(XVI)145089-2-d1810713-73-5API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-2-a | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (II)145089-2-a,(II)145089-2-e | 586-37-8 | 1-(3-Methoxyphenyl)ethanone |
| (III)145089-2-a | 122806-25-1 | (1E)-1-(3-Methoxyphenyl)ethanone oxime |
| (IV)145089-2-a | 62409-13-6 | 1-(3-Methoxyphenyl)ethanamine |
| (V)145089-2-a | 198756-81-9 | 1(S)-(3-Methoxyphenyl)ethylamine 2(S)-hydroxy-2-phenylacetate |
| (VI)145089-2-a,(VI)145089-2-c | 889443-69-0 | 1(S)-(3-Methoxyphenyl)-N,N-dimethylethylamine |
| (VIIa)145089-2-a | 139306-10-8 | (-)-3-((1S)-1-(Dimethylamino)ethyl)phenol |
| (VIIb)145089-2-a | - | Potassium 3-[(1S)-1-(dimethylamino)ethyl]phenolate |
| (VIIIa)145089-2-a | 42252-34-6 | N-Ethyl-N-methylcarbamic chloride |
| (VIIIb)145089-2-a | 928032-01-3 | Ethyl(methyl)carbamic bromide |
| (IX)145089-2-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
| (X)145089-2-a | - | 1(R)-(3-Methoxyphenyl)-N,N-dimethylethylamine 2(S)-hydroxy-2-phenylacetate |
| (XI)145089-2-a | 1071141-86-0 | 1(R)-(3-Methoxyphenyl)-N,N-dimethylethylamine |
| (XII)145089-2-a,(XII)145089-2-e | 120523-12-8 | (1R)-1-(3-Methoxyphenyl)ethanol |
| (XIII)145089-2-a | 1647103-52-3 | (1R)-1-(3-Methoxyphenyl)ethyl methanesulfonate |
| (XIV)145089-2-a | 124-40-3在售 | Dimethylamine anhydrous |
| (XV)145089-2-a | 1810713-46-2 | N-[(1Z)-1-(3-Methoxyphenyl)ethylidene]methanamine |
| (XVI)145089-2-a,(XVI)145089-2-d | 1810713-73-5 | N-Boc-[1(S)-(3-Methoxyphenyl)ethyl]-N-methylamine |
优化Route 8步骤 1 · 总收率 /
(VIIb)145089-2-a—(VIIIb)145089-2-a928032-01-3(XVII)145089-2-b—(XVIII)145089-2-b28249-49-2API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (VIIb)145089-2-a | - | Potassium 3-[(1S)-1-(dimethylamino)ethyl]phenolate |
| (VIIIb)145089-2-a | 928032-01-3 | Ethyl(methyl)carbamic bromide |
| (XVII)145089-2-b | - | 2,6-Diiododinaphtho[2,1-d:1',2'-f][1,3,2]dithiazepine 3,3,5,5-tetraoxide |
| (XVIII)145089-2-b | 28249-49-2 | (4-Methyl-3,5-dinitrophenyl)boronic acid |
优化Route 9步骤 4 · 总收率 /
(VI)145089-2-a,(VI)145089-2-c889443-69-0(XIX)145089-2-c,(XIX)145089-2-e23308-82-9(XX)145089-2-c343338-28-3(XXI)145089-2-c1304771-29-6(XXII)145089-2-c82796-69-8(XXIII)145089-2-c19164-77-3(XXIV)145089-2-c55-21-0(XXV)145089-2-c—(XXVI)145089-2-c67-56-1(XXVII)145089-2-c1786847-21-9(XXVIII)145089-2-c5824-40-8API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (VI)145089-2-a,(VI)145089-2-c | 889443-69-0 | 1(S)-(3-Methoxyphenyl)-N,N-dimethylethylamine |
| (XIX)145089-2-c,(XIX)145089-2-e | 23308-82-9 | (+/-)-3-Methoxy-alpha-methylbenzyl alcohol |
| (XX)145089-2-c | 343338-28-3在售 | (S)-(-)-2-Methyl-2-propanesulfinamide |
| (XXI)145089-2-c | 1304771-29-6 | (SS)-N-[(1S)-1-(3-Methoxyphenyl)ethyl]-2-methylpropane-2-sulfinamide |
| (XXII)145089-2-c | 82796-69-8 | (1S)-1-(3-Methoxyphenyl)ethanamine |
| (XXIII)145089-2-c | 19164-77-3 | 1-Ethyl-3-iodobenzene |
| (XXIV)145089-2-c | 55-21-0 | Benzamide |
| (XXV)145089-2-c | - | N-[(1S)-1-(3-Iodophenyl)ethyl]benzamide |
| (XXVI)145089-2-c | 67-56-1在售 | Hydroxymethane |
| (XXVII)145089-2-c | 1786847-21-9 | N-[(1S)-1-(3-Methoxyphenyl)ethyl]benzamide |
| (XXVIII)145089-2-c | 5824-40-8 | 1,1,1-Triphenylmethanamine |
优化Route 10步骤 3 · 总收率 /
(XVI)145089-2-a,(XVI)145089-2-d1810713-73-5(XXIX)145089-2-d—(XXX)145089-2-d917-64-6(XXXI)145089-2-d2679779-00-9(XXXII)145089-2-d218900-56-2(XXXIII)145089-2-d74-88-4API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XVI)145089-2-a,(XVI)145089-2-d | 1810713-73-5 | N-Boc-[1(S)-(3-Methoxyphenyl)ethyl]-N-methylamine |
| (XXIX)145089-2-d | - | (3aS,7aS)-2-[(E)-[(3-Methoxyphenyl)methylidene]amino]-1,3-di(propan-2-yl)octahydro-1H-1,3,2lambda5-benzodiazaphosphol-2-one |
| (XXX)145089-2-d | 917-64-6 | Iodo(methyl)magnesium |
| (XXXI)145089-2-d | 2679779-00-9 | (3aS,7aS)-2-[[(1S)-1-(3-Methoxyphenyl)ethyl]amino]-1,3-di(propan-2-yl)octahydro-1H-1,3,2lambda5-benzodiazaphosphol-2-one |
| (XXXII)145089-2-d | 218900-56-2 | N-Boc-1(S)-(3-Methoxyphenyl)ethanamine |
| (XXXIII)145089-2-d | 74-88-4在售 | Iodomethane |
优化Route 11步骤 3 · 总收率 /
(II)145089-2-a,(II)145089-2-e586-37-8(XII)145089-2-a,(XII)145089-2-e120523-12-8(XIX)145089-2-c,(XIX)145089-2-e23308-82-9(XXXIV)145089-2-e2413177-20-3API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (II)145089-2-a,(II)145089-2-e | 586-37-8 | 1-(3-Methoxyphenyl)ethanone |
| (XII)145089-2-a,(XII)145089-2-e | 120523-12-8 | (1R)-1-(3-Methoxyphenyl)ethanol |
| (XIX)145089-2-c,(XIX)145089-2-e | 23308-82-9 | (+/-)-3-Methoxy-alpha-methylbenzyl alcohol |
| (XXXIV)145089-2-e | 2413177-20-3 | 2-[[1-(3-Methoxyphenyl)ethoxy]carbonyl]benzoic acid |
优化Route 12步骤 5 · 总收率 /
(I)145089-4-a121-71-1(II)145089-4-a—(III)145089-4-a923035-06-7(IV)145089-4-a105601-04-5(V)145089-4-a63720-38-7(VI)145089-4-a,(VI)145089-4-b139306-10-8(VIIa)145089-4-a42252-34-6(VIIb)145089-4-a928032-01-3(VIII)145089-4-a123441-03-2API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-4-a | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (II)145089-4-a | - | Aminomethane |
| (III)145089-4-a | 923035-06-7 | 3-[1-(Methylamino)ethyl]phenol |
| (IV)145089-4-a | 105601-04-5 | 3-[1-(Dimethylamino)ethyl]phenol |
| (V)145089-4-a | 63720-38-7 | 3-(1-Aminoethyl)phenol |
| (VI)145089-4-a,(VI)145089-4-b | 139306-10-8 | (-)-3-((1S)-1-(Dimethylamino)ethyl)phenol |
| (VIIa)145089-4-a | 42252-34-6 | N-Ethyl-N-methylcarbamic chloride |
| (VIIb)145089-4-a | 928032-01-3 | Ethyl(methyl)carbamic bromide |
| (VIII)145089-4-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
优化Route 13步骤 4 · 总收率 /
(IX)145089-4-b173098-21-0(VI)145089-4-a,(VI)145089-4-b139306-10-8(X)145089-4-b215395-13-4(XI)145089-4-b124-40-3(XII)145089-4-b2484093-31-2(XIII)145089-4-b2484093-32-3API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (IX)145089-4-b | 173098-21-0 | 1-(Benzyloxy)-3-ethenylbenzene |
| (VI)145089-4-a,(VI)145089-4-b | 139306-10-8 | (-)-3-((1S)-1-(Dimethylamino)ethyl)phenol |
| (X)145089-4-b | 215395-13-4 | (2S)-2-[3-(Benzyloxy)phenyl]oxirane |
| (XI)145089-4-b | 124-40-3在售 | Dimethylamine anhydrous |
| (XII)145089-4-b | 2484093-31-2 | (2R)-2-[3-(Benzyloxy)phenyl]-2-(dimethylamino)ethan-1-ol |
| (XIII)145089-4-b | 2484093-32-3 | (2R)-2-[3-(Benzyloxy)phenyl]-2-(dimethylamino)ethyl methanesulfonate |
优化Route 14步骤 8 · 总收率 /
(I)145089-5-a121-71-1(II)145089-5-a58297-34-0(III)145089-5-a1492060-24-8(IV)145089-5-a1213234-35-5(V)145089-5-a63720-38-7(VI)145089-5-a1351944-50-7(VII)145089-5-a1213234-37-7(VIII)145089-5-a1213234-40-2(IX)145089-5-a139306-10-8(X)145089-5-a42252-34-6(XI)145089-5-a123441-03-2(XII)145089-5-a—(XIII)145089-5-a—API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-5-a | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (II)145089-5-a | 58297-34-0 | 3-Acetylphenyl 4-methylbenzenesulfonate |
| (III)145089-5-a | 1492060-24-8 | 3-[1-(Formylamino)ethyl]phenyl 4-methylbenzenesulfonate |
| (IV)145089-5-a | 1213234-35-5 | 3-(1-Aminoethyl)phenyl 4-methylbenzenesulfonate |
| (V)145089-5-a | 63720-38-7 | 3-(1-Aminoethyl)phenol |
| (VI)145089-5-a | 1351944-50-7 | 3-[(1R)-1-Aminoethyl]phenyl 4-methylbenzenesulfonate |
| (VII)145089-5-a | 1213234-37-7 | 3-[(1S)-1-Aminoethyl]phenyl 4-methylbenzenesulfonate |
| (VIII)145089-5-a | 1213234-40-2 | 3-[(1S)-1-(Dimethylamino)ethyl]phenyl 4-methylbenzenesulfonate |
| (IX)145089-5-a | 139306-10-8 | (-)-3-((1S)-1-(Dimethylamino)ethyl)phenol |
| (X)145089-5-a | 42252-34-6 | N-Ethyl-N-methylcarbamic chloride |
| (XI)145089-5-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
| (XII)145089-5-a | - | 3-[(1R)-1-[[(E)-Phenylmethylidene]amino]ethyl]phenyl 4-methylbenzenesulfonate |
| (XIII)145089-5-a | - | 3-(1-[[(E)-Phenylmethylidene]amino]ethyl)phenyl 4-methylbenzenesulfonate |
优化Route 15步骤 6 · 总收率 /
(I)145089-6-a121-71-1(II)145089-6-a2627-86-3(III)145089-6-a1017234-21-7(IV)145089-6-a1017234-23-9(V)145089-6-a894079-42-6(VI)145089-6-a139306-10-8(VII)145089-6-a624-78-2(VIIII)145089-6-a123441-03-2API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-6-a | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (II)145089-6-a | 2627-86-3 | (S)-(-)-1-Phenylethylamine |
| (III)145089-6-a | 1017234-21-7 | 3-[(1S)-1-[[(1S)-1-Phenylethyl]amino]ethyl]phenol |
| (IV)145089-6-a | 1017234-23-9 | 3-[(1S)-1-[Methyl[(1S)-1-phenylethyl]amino]ethyl]phenol |
| (V)145089-6-a | 894079-42-6 | 3-[1(S)-(Methylamino)ethyl]phenol |
| (VI)145089-6-a | 139306-10-8 | (-)-3-((1S)-1-(Dimethylamino)ethyl)phenol |
| (VII)145089-6-a | 624-78-2 | N-Ethyl-N-methylamine |
| (VIIII)145089-6-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
优化Route 16步骤 3 · 总收率 /
(I)145089-7-a586-37-8(II)145089-7-a122806-25-1(III)145089-7-a1384454-55-0(IV)145089-7-a82796-69-8API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-7-a | 586-37-8 | 1-(3-Methoxyphenyl)ethanone |
| (II)145089-7-a | 122806-25-1 | (1E)-1-(3-Methoxyphenyl)ethanone oxime |
| (III)145089-7-a | 1384454-55-0 | (1E)-N-(Benzyloxy)-1-(3-methoxyphenyl)ethanimine |
| (IV)145089-7-a | 82796-69-8 | (1S)-1-(3-Methoxyphenyl)ethanamine |
优化Route 17步骤 5 · 总收率 /
(Ia)145089-9-a1162673-62-2(Ib)145089-9-a90933-75-8(II)145089-9-a1412902-99-8(III)145089-9-a1412902-91-0(IV)145089-9-a1017234-23-9(V)145089-9-a42252-34-6(VI)145089-9-a1412902-83-0(VII)145089-9-a1017234-25-1(VIII)145089-9-a123441-03-2API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (Ia)145089-9-a | 1162673-62-2 | (1S)-1-(3-Methoxyphenyl)-N-methyl-N-[(1S)-1-phenylethyl]ethanamine |
| (Ib)145089-9-a | 90933-75-8 | (1S)-1-(3-Methoxyphenyl)-N-[(1S)-1-phenylethyl]ethanamine |
| (II)145089-9-a | 1412902-99-8 | (1S)-1-(3-Methoxyphenyl)-N,N-dimethyl-N-[(1S)-1-phenylethyl]ethanaminium iodide |
| (III)145089-9-a | 1412902-91-0 | (1S)-1-(3-Hydroxyphenyl)-N,N-dimethyl-N-[(1S)-1-phenylethyl]ethanaminium iodide |
| (IV)145089-9-a | 1017234-23-9 | 3-[(1S)-1-[Methyl[(1S)-1-phenylethyl]amino]ethyl]phenol |
| (V)145089-9-a | 42252-34-6 | N-Ethyl-N-methylcarbamic chloride |
| (VI)145089-9-a | 1412902-83-0 | (1S)-1-(3-[[Ethyl(methyl)carbamoyl]oxy]phenyl)-N,N-dimethyl-N-[(1S)-1-phenylethyl]ethanaminium iodide |
| (VII)145089-9-a | 1017234-25-1 | 3-[(1S)-1-[Methyl[(1S)-1-phenylethyl]amino]ethyl]phenyl ethyl(methyl)carbamate |
| (VIII)145089-9-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
优化Route 18步骤 6 · 总收率 /
(I)145089-11-a121-71-1(II)145089-11-a625852-10-0(III)145089-11-a1233378-72-7(IV)145089-11-a124-40-3(V)145089-11-a1233378-78-3(VI)145089-11-a139306-10-8(VII)145089-11-a42252-34-6(VIII)145089-11-a123441-03-2(IX)145089-11-a855300-09-3(X)145089-11-a856408-80-5(XI)145089-11-a1418318-99-6API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-11-a | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (II)145089-11-a | 625852-10-0 | 3-[1(R)-Hydroxyethyl]phenol |
| (III)145089-11-a | 1233378-72-7 | 3-[(1R)-1-[(Methanesulfonyl)oxy]ethyl]phenyl methanesulfonate |
| (IV)145089-11-a | 124-40-3在售 | Dimethylamine anhydrous |
| (V)145089-11-a | 1233378-78-3 | 3-[(1S)-1-(Dimethylamino)ethyl]phenyl methanesulfonate |
| (VI)145089-11-a | 139306-10-8 | (-)-3-((1S)-1-(Dimethylamino)ethyl)phenol |
| (VII)145089-11-a | 42252-34-6 | N-Ethyl-N-methylcarbamic chloride |
| (VIII)145089-11-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
| (IX)145089-11-a | 855300-09-3 | 3-Acetylphenyl ethyl(methyl)carbamate |
| (X)145089-11-a | 856408-80-5 | 3-[(1R)-1-Hydroxyethyl]phenyl ethyl(methyl)carbamate |
| (XI)145089-11-a | 1418318-99-6 | (1R)-1-(3-[[Ethyl(methyl)carbamoyl]oxy]phenyl)ethyl methanesulfonate |
优化Route 19步骤 1 · 总收率 /
(I)145089-14-a93351-40-7(II)145089-14-a1007894-87-2API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-14-a | 93351-40-7 | 1-(3-Methoxyphenyl)ethyl acetate |
| (II)145089-14-a | 1007894-87-2 | (1S)-1-(3-Methoxyphenyl)ethyl acetate |
优化Route 20步骤 1 · 总收率 /
(I)145089-15-a586-37-8(II)145089-15-a506-59-2(III)145089-15-a169772-44-5API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-15-a | 586-37-8 | 1-(3-Methoxyphenyl)ethanone |
| (II)145089-15-a | 506-59-2在售 | Dimethylamine hydrochloride |
| (III)145089-15-a | 169772-44-5 | 1-(3-Methoxyphenyl)-N,N-dimethylethanamine |
优化Route 21步骤 4 · 总收率 /
(I)145089-17-a121-71-1(II)145089-17-a—(III)145089-17-a—(IV)145089-17-a923035-06-7(V)145089-17-a894079-42-6(VI)145089-17-a139306-10-8API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-17-a | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (II)145089-17-a | - | Aminomethane |
| (III)145089-17-a | - | 3-[(1E)-N-Methylethanimidoyl]phenol |
| (IV)145089-17-a | 923035-06-7 | 3-[1-(Methylamino)ethyl]phenol |
| (V)145089-17-a | 894079-42-6 | 3-[1(S)-(Methylamino)ethyl]phenol |
| (VI)145089-17-a | 139306-10-8 | (-)-3-((1S)-1-(Dimethylamino)ethyl)phenol |
优化Route 22步骤 2 · 总收率 /
(I)145089-18-a2053896-43-6(II)145089-18-a1809788-66-6(III)145089-18-a190391-62-9API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-18-a | 2053896-43-6 | (1S)-N-[(1E)-1-[3-(Benzyloxy)phenyl]ethylidene]-1-phenylethanamine |
| (II)145089-18-a | 1809788-66-6 | (1S)-1-[3-(Benzyloxy)phenyl]-N-[(1S)-1-phenylethyl]ethanamine |
| (III)145089-18-a | 190391-62-9 | (1S)-1-[3-(Benzyloxy)phenyl]ethanamine |
优化Route 23步骤 7 · 总收率 /
(I)145089-19-a586-37-8(II)145089-19-a2627-86-3(III)145089-19-a90933-75-8(IV)145089-19-a1162673-62-2(V)145089-19-a1017234-23-9(VI)145089-19-a42252-34-6(VII)145089-19-a624-78-2(VIII)145089-19-a32315-10-9(IX)145089-19-a1017234-25-1(X)145089-19-a923035-05-6(XI)145089-19-a855300-09-3(XII)145089-19-a—(XIII)145089-19-a123441-03-2(XIV)145089-19-a2053896-45-8(XV)145089-19-a1056639-26-9API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-19-a | 586-37-8 | 1-(3-Methoxyphenyl)ethanone |
| (II)145089-19-a | 2627-86-3 | (S)-(-)-1-Phenylethylamine |
| (III)145089-19-a | 90933-75-8 | (1S)-1-(3-Methoxyphenyl)-N-[(1S)-1-phenylethyl]ethanamine |
| (IV)145089-19-a | 1162673-62-2 | (1S)-1-(3-Methoxyphenyl)-N-methyl-N-[(1S)-1-phenylethyl]ethanamine |
| (V)145089-19-a | 1017234-23-9 | 3-[(1S)-1-[Methyl[(1S)-1-phenylethyl]amino]ethyl]phenol |
| (VI)145089-19-a | 42252-34-6 | N-Ethyl-N-methylcarbamic chloride |
| (VII)145089-19-a | 624-78-2 | N-Ethyl-N-methylamine |
| (VIII)145089-19-a | 32315-10-9 | Bis(trichloromethyl) carbonate |
| (IX)145089-19-a | 1017234-25-1 | 3-[(1S)-1-[Methyl[(1S)-1-phenylethyl]amino]ethyl]phenyl ethyl(methyl)carbamate |
| (X)145089-19-a | 923035-05-6 | 3-[(1S)-1-(Methylamino)ethyl]phenyl ethyl(methyl)carbamate |
| (XI)145089-19-a | 855300-09-3 | 3-Acetylphenyl ethyl(methyl)carbamate |
| (XII)145089-19-a | - | Aminomethane |
| (XIII)145089-19-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
| (XIV)145089-19-a | 2053896-45-8 | 3-[(1E)-N-[(1S)-1-Phenylethyl]ethanimidoyl]phenyl ethyl(methyl)carbamate |
| (XV)145089-19-a | 1056639-26-9 | 3-[(1S)-1-[[(1S)-1-Phenylethyl]amino]ethyl]phenyl ethyl(methyl)carbamate |
优化Route 24步骤 4 · 总收率 /
(I)145089-20-a121-71-1(II)145089-20-a34068-01-4(III)145089-20-a2627-86-3(IV)145089-20-a2053896-43-6(V)145089-20-a1809788-66-6(VI)145089-20-a123982-81-0API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-20-a | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (II)145089-20-a | 34068-01-4 | 1-[3-(Benzyloxy)phenyl]ethanone |
| (III)145089-20-a | 2627-86-3 | (S)-(-)-1-Phenylethylamine |
| (IV)145089-20-a | 2053896-43-6 | (1S)-N-[(1E)-1-[3-(Benzyloxy)phenyl]ethylidene]-1-phenylethanamine |
| (V)145089-20-a | 1809788-66-6 | (1S)-1-[3-(Benzyloxy)phenyl]-N-[(1S)-1-phenylethyl]ethanamine |
| (VI)145089-20-a | 123982-81-0 | 3-[(1S)-1-Aminoethyl]phenol |
优化Route 25步骤 3 · 总收率 /
(I)145089-21-a,(I)145089-21-b855300-09-3(II)145089-21-a1257519-35-9(III)145089-21-a124-40-3(IV)145089-21-a123441-03-2(V)145089-21-a,(V)145089-21-b856408-80-5API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-21-a,(I)145089-21-b | 855300-09-3 | 3-Acetylphenyl ethyl(methyl)carbamate |
| (II)145089-21-a | 1257519-35-9 | 3-[(1S)-1-Hydroxyethyl]phenyl ethyl(methyl)carbamate |
| (III)145089-21-a | 124-40-3在售 | Dimethylamine anhydrous |
| (IV)145089-21-a | 123441-03-2 | (S)-3-(1-(Dimethylamino)ethyl)phenyl ethyl(methyl)carbamate |
| (V)145089-21-a,(V)145089-21-b | 856408-80-5 | 3-[(1R)-1-Hydroxyethyl]phenyl ethyl(methyl)carbamate |
优化Route 26步骤 4 · 总收率 /
(I)145089-21-a,(I)145089-21-b855300-09-3(V)145089-21-a,(V)145089-21-b856408-80-5(VI)145089-21-b121-71-1(VII)145089-21-b42252-34-6(VIII)145089-21-b1222073-98-4(IX)145089-21-b2413177-23-6API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-21-a,(I)145089-21-b | 855300-09-3 | 3-Acetylphenyl ethyl(methyl)carbamate |
| (V)145089-21-a,(V)145089-21-b | 856408-80-5 | 3-[(1R)-1-Hydroxyethyl]phenyl ethyl(methyl)carbamate |
| (VI)145089-21-b | 121-71-1 | 1-(3-Hydroxyphenyl)ethanone |
| (VII)145089-21-b | 42252-34-6 | N-Ethyl-N-methylcarbamic chloride |
| (VIII)145089-21-b | 1222073-98-4 | 3-(1-Hydroxyethyl)phenyl ethyl(methyl)carbamate |
| (IX)145089-21-b | 2413177-23-6 | 2-[[1-(3-[[Ethyl(methyl)carbamoyl]oxy]phenyl)ethoxy]carbonyl]benzoic acid |
优化Route 27步骤 4 · 总收率 /
(I)145089-25-a93-55-0(II)145089-25-a5470-11-1(III)145089-25-a—(IV)145089-25-a2890-85-9(V)145089-25-a57680-92-9(VI)145089-25-a3082-64-2API · 重酒石酸卡巴拉汀
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)145089-25-a | 93-55-0 | 1-Phenyl-1-propanone |
| (II)145089-25-a | 5470-11-1在售 | Amino alcohol hydrochloride |
| (III)145089-25-a | - | N-[1-Phenylpropylidene]hydroxylamine |
| (IV)145089-25-a | 2890-85-9 | N-[1-Phenylprop-1-en-1-yl]acetamide |
| (V)145089-25-a | 57680-92-9 | N-[(1R)-1-Phenylpropyl]acetamide |
| (VI)145089-25-a | 3082-64-2 | (R)-(+)-alpha-Ethylbenzylamine |
常见问题（FAQ）
重酒石酸卡巴拉汀的适应症有哪些？
已批准的适应症包括：阿尔茨海默病、痴呆、帕金森病。
重酒石酸卡巴拉汀的专利什么时候到期？
重酒石酸卡巴拉汀的专利到期年暂无公开口径，本页会在数据管道核实后更新。
重酒石酸卡巴拉汀有几条合成路线？
本站收录 27 条合成路线，最短路线 1 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
重酒石酸卡巴拉汀的关键中间体在哪里可以采购？
重酒石酸卡巴拉汀的多条路线中间体已挂接 CAS 档案，其中 6 个 CAS 已有优贝德（Unibest）供应网络在售报价，可在本页路线表中直接查看并询价。
如何获取重酒石酸卡巴拉汀中间体的报价？
在本页选择目标中间体的 CAS 进入档案页，或在询价页直接提交需求；CAS 会自动带入供需撮合流程，由供应网络反馈报价。
数据来源：多源数据交叉核实（仅结构化字段） · 2026-09-27