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秋水仙碱
Tier C · 观察 / 贸易Colchicine
URL Pharma Inc
原研
1995
首批上市
-
到期年（公开口径）
$0.53B ▲
峰值销售
化学药
类型
靶点：Tubulin
商品名：Colcrys、Colstat、Gloperba、Mitigare
适应症（已批准）：冠状动脉病变、心肌梗塞、中风、痛风性关节炎
各地区研发/上市状态
美国
临床三期
1993-09-01
欧盟
批准上市
2026-07-24
中国
批准上市
1995-01-01
日本
临床二期
2017-06-15
合成路线与中间体11 routes
原研路线 × 0优化路线（非专利）× 11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。
优化Route 1步骤 2 · 总收率 /
(I)70274-1-a—(II)70274-1-a66148-20-7(III)70274-1-a—(IV)70274-1-a—API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-1-a | - | N-(1,2,3,9,10-Pentamethoxy-5,6-dihydrobenzo[a]heptalen-7-yl)acetamide |
| (II)70274-1-a | 66148-20-7 | N-(1,2,3,10-Tetramethoxy-9-oxo-5,6,8,9-tetrahydrobenzo[a]heptalen-7-yl)acetamide |
| (III)70274-1-a | - | N-Acetyl-N-(1,2,3,9,10-pentamethoxy-5,6-dihydrobenzo[a]heptalen-7-yl)acetamide |
| (IV)70274-1-a | - | N-(1,2,3,10-Tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl)acetamide |
优化Route 2步骤 8 · 总收率 /
(I)70274-2-a—(II)70274-2-a39053-78-6(III)70274-2-a5320-31-0(IV)70274-2-a—(V)70274-2-a—(VI)70274-2-a20374-70-3(VII)70274-2-a—(VIII)70274-2-a7101-38-4(IX)70274-2-a5320-48-9(X)70274-2-a—API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-2-a | - | (3,4,5-Trimethoxyphenyl)acetic acid |
| (II)70274-2-a | 39053-78-6 | (3,4,5-Trimethoxyphenyl)acetyl chloride |
| (III)70274-2-a | 5320-31-0 | (3,4,5-Trimethoxyphenyl)acetaldehyde |
| (IV)70274-2-a | - | 3,8-Dihydroxycyclohepta[c]pyran-1,9-dione |
| (V)70274-2-a | - | 8-Hydroxy-3-(3,4,5-trimethoxybenzyl)-3,4-dihydrocyclohepta[c]pyran-1,9-dione |
| (VI)70274-2-a | 20374-70-3 | 2-Hydroxy-6-[(2Z)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-yl]cyclohepta-2,4,6-trien-1-one |
| (VII)70274-2-a | - | 2-Hydroxy-6-[3-(3,4,5-trimethoxyphenyl)propyl]cyclohepta-2,4,6-trien-1-one |
| (VIII)70274-2-a | 7101-38-4 | 2-Hydroxy-6-[3-(3,4,5-trihydroxyphenyl)propyl]cyclohepta-2,4,6-trien-1-one |
| (IX)70274-2-a | 5320-48-9 | 1,2,3,10-Tetrahydroxy-6,7-dihydrobenzo[a]heptalen-9(5H)-one |
| (X)70274-2-a | - | 10-Hydroxy-1,2,3-trimethoxy-6,7-dihydrobenzo[a]heptalen-9(5H)-one |
优化Route 3步骤 8 · 总收率 /
(XI)70274-3-a—(I)70274-3-a3596-71-2(II)70274-3-a107-13-1(III)70274-3-a49562-02-9(IV)70274-3-a96-32-2(V)70274-3-a94877-09-5(VI)70274-3-a94440-92-3(VII)70274-3-a99711-41-8(VIII)70274-3-a99831-21-7(IX)70274-3-a—(X)70274-3-a1098-19-7API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XI)70274-3-a | - | 10-Hydroxy-1,2,3-trimethoxy-6,7-dihydrobenzo[a]heptalen-9(5H)-one |
| (I)70274-3-a | 3596-71-2 | 2,3,4-Trimethoxy-5,7,8,9-tetrahydro-6H-benzocyclohepten-6-one |
| (II)70274-3-a | 107-13-1 | 2-Propenonitrile |
| (III)70274-3-a | 49562-02-9 | 3-(2,3,4-Trimethoxy-6-oxo-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-yl)propanenitrile |
| (IV)70274-3-a | 96-32-2 | 2-Bromoacetic acid methyl ester |
| (V)70274-3-a | 94877-09-5 | Methyl [5-(2-cyanoethyl)-6-hydroxy-2,3,4-trimethoxy-6,7,8,9-tetrahydro-5H-benzocyclohepten-6-yl]acetate |
| (VI)70274-3-a | 94440-92-3 | 3-[6-(Carboxymethyl)-6-hydroxy-2,3,4-trimethoxy-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-yl]propanoic acid |
| (VII)70274-3-a | 99711-41-8 | Methyl (9,10,11-trimethoxy-3-oxo-2,3,5,6,7,11b-hexahydrobenzo[3,4]cyclohepta[1,2-b]pyran-4a(1H)-yl)acetate |
| (VIII)70274-3-a | 99831-21-7 | 1,2,3-Trimethoxy-5,6,7,8,9,11,12,12a-octahydro-10H-7a,10-epoxybenzo[a]heptalene-9,10-diol |
| (IX)70274-3-a | - | 7a-Hydroxy-1,2,3-trimethoxy-5,6,7,7a,8,11,12,12a-octahydrobenzo[a]heptalene-9,10-dione |
| (X)70274-3-a | 1098-19-7 | 9-Hydroxy-1,2,3-trimethoxy-6,7,11,12-tetrahydrobenzo[a]heptalen-10(5H)-one |
优化Route 4步骤 4 · 总收率 /
(I)70274-4-a206195-34-8(II)70274-4-a131120-05-3(III)70274-4-a206195-19-9(IV)70274-4-a186374-95-8(V)70274-4-a3476-50-4(VI)70274-4-a108-24-7API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-4-a | 206195-34-8 | tert-Butyl [(4S)-8,9,10-trimethoxy-5,6-dihydro-4H-benzo[3,4]cyclohepta[1,2-b]furan-4-yl]carbamate |
| (II)70274-4-a | 131120-05-3 | [(3,3-Dimethoxyprop-1-en-2-yl)oxy](trimethyl)silane |
| (III)70274-4-a | 206195-19-9 | tert-Butyl [(7S,7aR,10S,11R)-1,2,3,10-tetramethoxy-9-oxo-6,7,8,9,10,11-hexahydro-5H-7a,11-epoxybenzo[a]heptalen-7-yl]carbamate |
| (IV)70274-4-a | 186374-95-8 | tert-Butyl [(7S)-1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]carbamate |
| (V)70274-4-a | 3476-50-4 | - |
| (VI)70274-4-a | 108-24-7 | Acetic acid acetic anhydride |
优化Route 5步骤 2 · 总收率 /
(I)70274-5-a—(II)70274-5-a—(III)70274-5-a—(IV)70274-5-a478361-89-6API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-5-a | - | (5R)-5-Hydroxy-2,2,9,10,11-pentamethoxy-2,5,6,7-tetrahydro-3H-dibenzo[a,c][7]annulen-3-one |
| (II)70274-5-a | - | [Dimethyl(oxido)-lambda6-sulfanylidene]methane |
| (III)70274-5-a | - | (4R)-4-Hydroxy-1,1,8,9,10-pentamethoxy-5,6,11,11a-tetrahydro-1H-benzo[a]cyclopropa[1,6]benzo[1,2-c][7]annulen-2(4H)-one |
| (IV)70274-5-a | 478361-89-6 | (7R)-7-Hydroxy-1,2,3,10-tetramethoxy-6,7-dihydrobenzo[a]heptalen-9(5H)-one |
优化Route 6步骤 4 · 总收率 /
(I)70274-6-a56177-98-1(II)70274-6-a56178-02-0(III)70274-6-a—(IV)70274-6-a—(V)70274-6-a1935-02-0API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-6-a | 56177-98-1 | 2-Methoxy-4-[3-(3,4,5-trimethoxyphenyl)propyl]phenol |
| (II)70274-6-a | 56178-02-0 | 3,6',7',8'-Tetramethoxy-3',4'-dihydro-2'H,4H-spiro[cyclohexa-2,5-diene-1,1'-naphthalen]-4-one |
| (III)70274-6-a | - | 3,6',7',8'-Tetramethoxy-3',4'-dihydro-2'H-spiro[cyclohexa-2,5-diene-1,1'-naphthalen]-4-ol |
| (IV)70274-6-a | - | 4,6',7',8'-Tetramethoxy-3',4'-dihydro-2'H,5H-spiro[bicyclo[4.1.0]hept-3-ene-2,1'-naphthalen]-5-one |
| (V)70274-6-a | 1935-02-0 | 1,2,3,9-Tetramethoxy-6,7-dihydrobenzo[a]heptalen-10(5H)-one |
优化Route 7步骤 7 · 总收率 /
(I)70274-7-a2103-57-3(II)70274-7-a193634-77-4(III)70274-7-a2301968-36-3(IV)70274-7-a—(V)70274-7-a90965-06-3(VI)70274-7-a2146098-52-2(VII)70274-7-a98-00-0(VIII)70274-7-a2146101-86-0(IX)70274-7-a196929-78-9(X)70274-7-a—(XI)70274-7-a—(XII)70274-7-a,(XII)70274-7-b—(XVIIIa)70274-7-b2301968-38-5(XXa)70274-7-b616-38-6API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-7-a | 2103-57-3 | 2,3,4-Trimethoxybenzaldehyde |
| (II)70274-7-a | 193634-77-4 | N-Methoxy-N-methylprop-2-enamide |
| (III)70274-7-a | 2301968-36-3 | (2E)-3-(2-Formyl-3,4,5-trimethoxyphenyl)-N-methoxy-N-methylprop-2-enamide |
| (IV)70274-7-a | - | 3-(2-Formyl-3,4,5-trimethoxyphenyl)-N-methoxy-N-methylpropanamide |
| (V)70274-7-a | 90965-06-3 | 1-(Dimethoxyphosphoryl)-2-oxopropane-1-diazonium |
| (VI)70274-7-a | 2146098-52-2 | 3-(2-Ethynyl-3,4,5-trimethoxyphenyl)-N-methoxy-N-methylpropanamide |
| (VII)70274-7-a | 98-00-0 | 2-(Hydroxymethyl)furan |
| (VIII)70274-7-a | 2146101-86-0 | 3-(2-Ethynyl-3,4,5-trimethoxyphenyl)-1-[5-(hydroxymethyl)furan-2-yl]propan-1-one |
| (IX)70274-7-a | 196929-78-9 | (R)-(+)-2-Methyl-2-propanesulfinamide |
| (X)70274-7-a | - | tert-Butyl[(Z)-[3-(2-ethynyl-3,4,5-trimethoxyphenyl)-1-[5-(hydroxymethyl)furan-2-yl]propylidene]amino]sulfaniumolate |
| (XI)70274-7-a | - | tert-Butyl([(1S)-3-(2-ethynyl-3,4,5-trimethoxyphenyl)-1-[5-(hydroxymethyl)furan-2-yl]propyl]amino)sulfaniumolate |
| (XII)70274-7-a,(XII)70274-7-b | - | [5-[(1S)-1-Amino-3-(2-ethynyl-3,4,5-trimethoxyphenyl)propyl]furan-2-yl]methanol |
| (XVIIIa)70274-7-b | 2301968-38-5 | N-[(7S,7aR,10S,11R)-9-Iodo-1,2,3,10-tetramethoxy-6,7,10,11-tetrahydro-5H-7a,11-epoxybenzo[a]heptalen-7-yl]acetamide |
| (XXa)70274-7-b | 616-38-6 | Carbonic acid dimethyl diester |
优化Route 8步骤 6 · 总收率 /
(XII)70274-7-a,(XII)70274-7-b—(XIII)70274-7-b108-24-7(XIV)70274-7-b2146098-53-3(XIX)70274-7-b2122830-53-7(XV)70274-7-b2122830-51-5(XVI)70274-7-b2301968-37-4(XVII)70274-7-b74-88-4(XVIIIa)70274-7-b2301968-38-5(XVIIIb)70274-7-b2122830-52-6(XXa)70274-7-b616-38-6(XXb)70274-7-b77-78-1API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XII)70274-7-a,(XII)70274-7-b | - | [5-[(1S)-1-Amino-3-(2-ethynyl-3,4,5-trimethoxyphenyl)propyl]furan-2-yl]methanol |
| (XIII)70274-7-b | 108-24-7 | Acetic acid acetic anhydride |
| (XIV)70274-7-b | 2146098-53-3 | N-[(1S)-3-(2-Ethynyl-3,4,5-trimethoxyphenyl)-1-[5-(hydroxymethyl)furan-2-yl]propyl]acetamide |
| (XIX)70274-7-b | 2122830-53-7 | N-[(7S,7aR,10S,11R)-1,2,3,10-Tetramethoxy-9-oxo-6,7,8,9,10,11-hexahydro-5H-7a,11-epoxybenzo[a]heptalen-7-yl]acetamide |
| (XV)70274-7-b | 2122830-51-5 | N-[(7S,7aR,11R)-1,2,3-Trimethoxy-10-oxo-6,7,10,11-tetrahydro-5H-7a,11-epoxybenzo[a]heptalen-7-yl]acetamide |
| (XVI)70274-7-b | 2301968-37-4 | N-[(7S,7aR,11R)-9-Iodo-1,2,3-trimethoxy-10-oxo-6,7,10,11-tetrahydro-5H-7a,11-epoxybenzo[a]heptalen-7-yl]acetamide |
| (XVII)70274-7-b | 74-88-4在售 | Iodomethane |
| (XVIIIa)70274-7-b | 2301968-38-5 | N-[(7S,7aR,10S,11R)-9-Iodo-1,2,3,10-tetramethoxy-6,7,10,11-tetrahydro-5H-7a,11-epoxybenzo[a]heptalen-7-yl]acetamide |
| (XVIIIb)70274-7-b | 2122830-52-6 | N-[(7S,7aR,10R,11R)-1,2,3,10-Tetramethoxy-6,7,10,11-tetrahydro-5H-7a,11-epoxybenzo[a]heptalen-7-yl]acetamide |
| (XXa)70274-7-b | 616-38-6 | Carbonic acid dimethyl diester |
| (XXb)70274-7-b | 77-78-1在售 | Sulfuric acid dimethyl diester |
优化Route 9步骤 7 · 总收率 /
(I)70274-8-a,(I)70274-8-b621-59-0(II)70274-8-a1826-67-1(III)70274-8-a2228434-21-5(IV)70274-8-a60-35-5(V)70274-8-a2434840-46-5(VI)70274-8-a2675-79-8(VII)70274-8-a2434840-47-6(VIII)70274-8-a,(VIII)70274-8-b2629878-75-5(IX)70274-8-a2434840-49-8(X)70274-8-a1774-47-6(XI)70274-8-a2629878-76-6API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-8-a,(I)70274-8-b | 621-59-0 | 3-Hydroxy-4-anisaldehyde |
| (II)70274-8-a | 1826-67-1 | (Vinyl)magnesium bromide |
| (III)70274-8-a | 2228434-21-5 | 5-(1-Hydroxyprop-2-en-1-yl)-2-methoxyphenol |
| (IV)70274-8-a | 60-35-5 | acetamide |
| (V)70274-8-a | 2434840-46-5 | N-[(1S)-1-(3-Hydroxy-4-methoxyphenyl)prop-2-en-1-yl]acetamide |
| (VI)70274-8-a | 2675-79-8 | 1-Bromo-3,4,5-trimethoxybenzene |
| (VII)70274-8-a | 2434840-47-6 | N-[(1S)-1-(3-Hydroxy-4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)propyl]acetamide |
| (VIII)70274-8-a,(VIII)70274-8-b | 2629878-75-5 | N-[(5S)-3-Hydroxy-2,9,10,11-tetramethoxy-6,7-dihydro-5H-dibenzo[a,c][7]annulen-5-yl]acetamide |
| (IX)70274-8-a | 2434840-49-8 | N-[(5S)-2,2,9,10,11-Pentamethoxy-3-oxo-3,5,6,7-tetrahydro-2H-dibenzo[a,c][7]annulen-5-yl]acetamide |
| (X)70274-8-a | 1774-47-6 | Trimethyl sulfoxide iodide |
| (XI)70274-8-a | 2629878-76-6 | N-[(4S,10bR,11aR)-1,1,8,9,10-Pentamethoxy-2-oxo-2,4,5,6,11,11a-hexahydro-1H-benzo[a]cyclopropa[1,6]benzo[1,2-c][7]annulen-4-yl]acetamide |
优化Route 10步骤 7 · 总收率 /
(I)70274-8-a,(I)70274-8-b621-59-0(VIII)70274-8-a,(VIII)70274-8-b2629878-75-5(XII)70274-8-b86-81-7(XIII)70274-8-b—(XIV)70274-8-b162442-15-1(XIX)70274-8-b—(XV)70274-8-b—(XVI)70274-8-b196929-78-9(XVII)70274-8-b—(XVIII)70274-8-b—(XX)70274-8-b75-36-5API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-8-a,(I)70274-8-b | 621-59-0 | 3-Hydroxy-4-anisaldehyde |
| (VIII)70274-8-a,(VIII)70274-8-b | 2629878-75-5 | N-[(5S)-3-Hydroxy-2,9,10,11-tetramethoxy-6,7-dihydro-5H-dibenzo[a,c][7]annulen-5-yl]acetamide |
| (XII)70274-8-b | 86-81-7 | 3,4,5-Trimethoxybenzaldehyde |
| (XIII)70274-8-b | - | 1-(3-Hydroxy-4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one |
| (XIV)70274-8-b | 162442-15-1 | 1-(3-Hydroxy-4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)propan-1-one |
| (XIX)70274-8-b | - | tert-Butyl[[(5S)-3-hydroxy-2,9,10,11-tetramethoxy-6,7-dihydro-5H-dibenzo[a,c][7]annulen-5-yl]amino]sulfaniumolate |
| (XV)70274-8-b | - | 1-[3-(Benzyloxy)-4-methoxyphenyl]-3-(3,4,5-trimethoxyphenyl)propan-1-one |
| (XVI)70274-8-b | 196929-78-9 | (R)-(+)-2-Methyl-2-propanesulfinamide |
| (XVII)70274-8-b | - | [[(1S)-1-[3-(Benzyloxy)-4-methoxyphenyl]-3-(3,4,5-trimethoxyphenyl)propyl]amino](tert-butyl)sulfaniumolate |
| (XVIII)70274-8-b | - | tert-Butyl[[(1S)-1-(3-hydroxy-4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)propyl]amino]sulfaniumolate |
| (XX)70274-8-b | 75-36-5 | Acetic acid chloride |
优化Route 11步骤 2 · 总收率 /
(I)70274-9-a—(II)70274-9-a7336-33-6(III)70274-9-a66-27-3(IV)70274-9-a124-63-0(V)70274-9-a67-56-1API · 秋水仙碱
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)70274-9-a | - | N-[(7S)-3-(beta-D-Glucopyranosyloxy)-1,2,10-trimethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide |
| (II)70274-9-a | 7336-33-6 | 3-Desmethylcolchicine |
| (III)70274-9-a | 66-27-3 | Methanesulfonic acid methyl ester |
| (IV)70274-9-a | 124-63-0 | Mesyl chloride |
| (V)70274-9-a | 67-56-1在售 | Hydroxymethane |
常见问题（FAQ）
秋水仙碱的适应症有哪些？
已批准的适应症包括：冠状动脉病变、心肌梗塞、中风、痛风性关节炎。
秋水仙碱的专利什么时候到期？
秋水仙碱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。
秋水仙碱有几条合成路线？
本站收录 11 条合成路线，最短路线 2 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
秋水仙碱的关键中间体在哪里可以采购？
秋水仙碱的多条路线中间体已挂接 CAS 档案，其中 3 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。
如何获取秋水仙碱中间体的报价？
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） · 2026-10-04