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洛替拉纳
Tier C · 观察 / 贸易Lotilaner
Elanco Tiergesundheit Ag
原研
2023
首批上市
-
到期年（公开口径）
无销量数据
峰值销售
化学药
类型
靶点：mites GABA-gated chloride channel
商品名：XDEMVY
适应症（已批准）：蠕形螨性睑缘炎
各地区研发/上市状态
美国
批准上市
2023-07-24
欧盟
-
中国
批准上市
2026-03-17
日本
-
合成路线与中间体8 routes
原研路线 × 0优化路线（非专利）× 8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 8 · 总收率 /
(I)700647-1-a14282-78-1(II)700647-1-a1862972-98-2(III)700647-1-a75-16-1(IV)700647-1-a13679-73-7(IX)700647-1-a—(V)700647-1-a,(V)700647-1-d859199-06-7(VI)700647-1-a,(VI)700647-1-d158401-00-4(VII)700647-1-a,(VII)700647-1-d—(VIII)700647-1-a,(VIII)700647-1-d5470-11-1(X)700647-1-a—(XI)700647-1-a,(XI)700647-1-d—(XII)700647-1-a,(XII)700647-1-b1171331-39-7(XIII)700647-1-a,(XIII)700647-1-c21928-51-8(XIV)700647-1-a—(XV)700647-1-a1547-87-1API · 洛替拉纳
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)700647-1-a | 14282-78-1在售 | 4-Methylthiophene-2-carboxylic acid |
| (II)700647-1-a | 1862972-98-2在售 | N-Methoxy-N,4-dimethylthiophene-2-carboxamide |
| (III)700647-1-a | 75-16-1在售 | Bromo(methyl)magnesium |
| (IV)700647-1-a | 13679-73-7在售 | 1-(4-Methylthiophen-2-yl)ethan-1-one |
| (IX)700647-1-a | - | 3-(5-Bromo-4-methylthiophen-2-yl)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazole |
| (V)700647-1-a,(V)700647-1-d | 859199-06-7在售 | 1-(5-Bromo-4-methylthiophen-2-yl)ethan-1-one |
| (VI)700647-1-a,(VI)700647-1-d | 158401-00-4在售 | 2,2,2-Trifluoro-1-(3,4,5-trichlorophenyl)ethan-1-one |
| (VII)700647-1-a,(VII)700647-1-d | - | 1-(5-Bromo-4-methylthiophen-2-yl)-4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-en-1-one |
| (VIII)700647-1-a,(VIII)700647-1-d | 5470-11-1在售 | Amino alcohol hydrochloride |
| (X)700647-1-a | - | 3-Methyl-5-[5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylic acid |
| (XI)700647-1-a,(XI)700647-1-d | - | 3-Methyl-5-[(5S)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylic acid |
| (XII)700647-1-a,(XII)700647-1-b | 1171331-39-7在售 | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide hydrochloride |
| (XIII)700647-1-a,(XIII)700647-1-c | 21928-51-8在售 | 5-Bromo-1,2,3-trichlorobenzene |
| (XIV)700647-1-a | - | (3,4,5-Trichlorophenyl)magnesium bromide |
| (XV)700647-1-a | 1547-87-1在售 | 2,2,2-Trifluoro-N,N-dimethylacetamide |
优化Route 2步骤 3 · 总收率 /
(XII)700647-1-a,(XII)700647-1-b1171331-39-7(XIX)700647-1-b142955-50-8(XVIa)700647-1-b1138-80-3(XVIb)700647-1-b4530-20-5(XVIIa)700647-1-b373-88-6(XVIIb)700647-1-b753-90-2(XVIIIa)700647-1-b1371632-79-9(XVIIIb)700647-1-b1231755-15-9(XX)700647-1-b79-04-9(XXI)700647-1-b170655-44-4(XXII)700647-1-b103-49-1(XXIII)700647-1-b—API · 洛替拉纳
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XII)700647-1-a,(XII)700647-1-b | 1171331-39-7在售 | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide hydrochloride |
| (XIX)700647-1-b | 142955-50-8在售 | 2,5-Dioxo-3-oxazolidinecarboxylic acid 1,1-dimethylethyl ester |
| (XVIa)700647-1-b | 1138-80-3在售 | 2-(Benzyloxycarbonylamino)acetic acid |
| (XVIb)700647-1-b | 4530-20-5在售 | 2-((tert-Butoxycarbonyl)amino)acetic acid |
| (XVIIa)700647-1-b | 373-88-6在售 | 2-Amino-1,1,1-trifluoroethane hydrochloride |
| (XVIIb)700647-1-b | 753-90-2在售 | 2-Amino-1,1,1-trifluoroethane |
| (XVIIIa)700647-1-b | 1371632-79-9在售 | Benzyl [2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]carbamate |
| (XVIIIb)700647-1-b | 1231755-15-9在售 | [(2,2,2-Trifluoroethylcarbamoyl)methyl]carbamic acid tert-butyl ester |
| (XX)700647-1-b | 79-04-9在售 | 2-Chloranylethanoyl chloride |
| (XXI)700647-1-b | 170655-44-4在售 | 2-Chloro-N-(2,2,2-trifluoroethyl)acetamide |
| (XXII)700647-1-b | 103-49-1在售 | (N-Benzylaminomethyl)benzene |
| (XXIII)700647-1-b | - | 2-(Dibenzylamino)-N-(2,2,2-trifluoroethyl)acetamide |
优化Route 3步骤 3 · 总收率 /
(XIII)700647-1-a,(XIII)700647-1-c21928-51-8(XXIV)700647-1-c63-74-1(XXV)700647-1-c22134-75-4(XXVI)700647-1-c697-88-1(XXVII)700647-1-c62-53-3(XXVIII)700647-1-c106-40-1API · 洛替拉纳
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XIII)700647-1-a,(XIII)700647-1-c | 21928-51-8在售 | 5-Bromo-1,2,3-trichlorobenzene |
| (XXIV)700647-1-c | 63-74-1在售 | 4-(Aminosulfonyl)aniline |
| (XXV)700647-1-c | 22134-75-4在售 | 3,5-Dichlorosulfanilamide |
| (XXVI)700647-1-c | 697-88-1在售 | (4-Bromo-2,6-dichlorophenyl)amine |
| (XXVII)700647-1-c | 62-53-3在售 | Aminobenzene |
| (XXVIII)700647-1-c | 106-40-1在售 | p-Bromoaniline |
优化Route 4步骤 7 · 总收率 /
(V)700647-1-a,(V)700647-1-d859199-06-7(VI)700647-1-a,(VI)700647-1-d158401-00-4(VII)700647-1-a,(VII)700647-1-d—(VIII)700647-1-a,(VIII)700647-1-d5470-11-1(XI)700647-1-a,(XI)700647-1-d—(XXIX)700647-1-d—(XXX)700647-1-d—(XXXI)700647-1-d—(XXXII)700647-1-d,(XXXII)700647-1-e2758907-87-6(XXXIII)700647-1-d—(XXXIV)700647-1-d7803-49-8(XXXV)700647-1-d—(XXXVI)700647-1-d—API · 洛替拉纳
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (V)700647-1-a,(V)700647-1-d | 859199-06-7在售 | 1-(5-Bromo-4-methylthiophen-2-yl)ethan-1-one |
| (VI)700647-1-a,(VI)700647-1-d | 158401-00-4在售 | 2,2,2-Trifluoro-1-(3,4,5-trichlorophenyl)ethan-1-one |
| (VII)700647-1-a,(VII)700647-1-d | - | 1-(5-Bromo-4-methylthiophen-2-yl)-4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-en-1-one |
| (VIII)700647-1-a,(VIII)700647-1-d | 5470-11-1在售 | Amino alcohol hydrochloride |
| (XI)700647-1-a,(XI)700647-1-d | - | 3-Methyl-5-[(5S)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylic acid |
| (XXIX)700647-1-d | - | 2-(5-Bromo-4-methylthiophen-2-yl)-2-methyl-1,3-dioxolane |
| (XXX)700647-1-d | - | 3-Methyl-5-(2-methyl-1,3-dioxolan-2-yl)thiophene-2-carboxylic acid |
| (XXXI)700647-1-d | - | Methyl 3-methyl-5-(2-methyl-1,3-dioxolan-2-yl)thiophene-2-carboxylate |
| (XXXII)700647-1-d,(XXXII)700647-1-e | 2758907-87-6在售 | Methyl 5-acetyl-3-methylthiophene-2-carboxylate |
| (XXXIII)700647-1-d | - | Methyl 3-methyl-5-[4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-enoyl]thiophene-2-carboxylate |
| (XXXIV)700647-1-d | 7803-49-8在售 | Amine N-oxide |
| (XXXV)700647-1-d | - | Methyl 3-methyl-5-[(5S)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylate |
| (XXXVI)700647-1-d | - | (5S)-3-(5-Bromo-4-methylthiophen-2-yl)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazole |
优化Route 5步骤 2 · 总收率 /
(XXXII)700647-1-d,(XXXII)700647-1-e2758907-87-6(XXXIX)700647-1-e2758907-91-2(XXXVII)700647-1-e23806-24-8(XXXVIII)700647-1-e78191-00-1API · 洛替拉纳
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XXXII)700647-1-d,(XXXII)700647-1-e | 2758907-87-6在售 | Methyl 5-acetyl-3-methylthiophene-2-carboxylate |
| (XXXIX)700647-1-e | 2758907-91-2在售 | 5-Acetyl-3-methylthiophene-2-carboxylic acid |
| (XXXVII)700647-1-e | 23806-24-8在售 | 2-Carboxy-3-methylthiophene |
| (XXXVIII)700647-1-e | 78191-00-1在售 | N-Acetyl-N,O-dimethylhydroxylamine |
优化Route 6步骤 5 · 总收率 /
(I)700647-2-a1368183-08-7(II)700647-2-a5470-11-1(III)700647-2-a2382920-59-2(IV)700647-2-a359821-38-8(V)700647-2-a—(VI)700647-2-a—(VII)700647-2-a—(VIII)700647-2-a—(IX)700647-2-a864736-87-8(X)700647-2-a—API · 洛替拉纳
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)700647-2-a | 1368183-08-7在售 | 5-Formyl-3-methylthiophene-2-carboxylic acid |
| (II)700647-2-a | 5470-11-1在售 | Amino alcohol hydrochloride |
| (III)700647-2-a | 2382920-59-2在售 | 5-[(Hydroxyimino)methyl]-3-methylthiophene-2-carboxylic acid |
| (IV)700647-2-a | 359821-38-8在售 | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide |
| (V)700647-2-a | - | 5-[(Hydroxyimino)methyl]-3-methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]thiophene-2-carboxamide |
| (VI)700647-2-a | - | 5-Formyl-3-methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]thiophene-2-carboxamide |
| (VII)700647-2-a | - | N-Hydroxy-4-methyl-5-([2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]carbamoyl)thiophene-2-carboximidoyl chloride |
| (VIII)700647-2-a | - | 4-Methyl-5-([2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]carbamoyl)thiophene-2-carbonitrile oxide |
| (IX)700647-2-a | 864736-87-8在售 | 1,2,3-Trichloro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene |
| (X)700647-2-a | - | (±)-3-Methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-5-[5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxamide |
优化Route 7步骤 6 · 总收率 /
(I)700647-3-a5834-16-2(II)700647-3-a38239-46-2(III)700647-3-a38239-45-1(IV)700647-3-a75-52-5(V)700647-3-a2624121-17-9(VI)700647-3-a—(VII)700647-3-a864736-87-8(VIII)700647-3-a—(IX)700647-3-a1171331-39-7API · 洛替拉纳
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)700647-3-a | 5834-16-2在售 | 2-Formyl-3-methylthiophene |
| (II)700647-3-a | 38239-46-2在售 | 5-Bromo-3-methylthiophene-2-carbaldehyde |
| (III)700647-3-a | 38239-45-1在售 | 5-Bromo-3-methylthiophene-2-carboxylic acid |
| (IV)700647-3-a | 75-52-5在售 | Nitrocarbol |
| (V)700647-3-a | 2624121-17-9在售 | 3-Methyl-5-(nitromethyl)thiophene-2-carboxylic acid |
| (VI)700647-3-a | - | 5-Carboxy-4-methylthiophene-2-carbonitrile oxide |
| (VII)700647-3-a | 864736-87-8在售 | 1,2,3-Trichloro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene |
| (VIII)700647-3-a | - | 3-Methyl-5-[5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylic acid |
| (IX)700647-3-a | 1171331-39-7在售 | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide hydrochloride |
优化Route 8步骤 4 · 总收率 /
(I)700647-4-a158401-00-4(II)700647-4-a859199-06-7(III)700647-4-a—(IV)700647-4-a—(V)700647-4-a1171331-39-7(VI)700647-4-a—(VII)700647-4-a7803-49-8API · 洛替拉纳
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)700647-4-a | 158401-00-4在售 | 2,2,2-Trifluoro-1-(3,4,5-trichlorophenyl)ethan-1-one |
| (II)700647-4-a | 859199-06-7在售 | 1-(5-Bromo-4-methylthiophen-2-yl)ethan-1-one |
| (III)700647-4-a | - | 1-(5-Bromo-4-methylthiophen-2-yl)-4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-en-1-one |
| (IV)700647-4-a | - | 3-Methyl-5-[4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-enoyl]thiophene-2-carboxylic acid |
| (V)700647-4-a | 1171331-39-7在售 | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide hydrochloride |
| (VI)700647-4-a | - | 3-Methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-5-[4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-enoyl]thiophene-2-carboxamide |
| (VII)700647-4-a | 7803-49-8在售 | Amine N-oxide |
常见问题（FAQ）
洛替拉纳的适应症有哪些？
已批准的适应症包括：蠕形螨性睑缘炎。
洛替拉纳的专利什么时候到期？
洛替拉纳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。
洛替拉纳有几条合成路线？
本站收录 8 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。
洛替拉纳的关键中间体在哪里可以采购？
洛替拉纳的多条路线中间体已挂接 CAS 档案，其中 39 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。
如何获取洛替拉纳中间体的报价？
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