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依林奈坦
Tier C · 观察 / 贸易Elinzanetant
葛兰素史克
原研
2025
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：NK1R、NK3R
商品名：Lynkuet
适应症（已批准）：热潮红、血管舒缩症
各地区研发/上市状态
美国
批准上市
2025-10-24
欧盟
批准上市
2025-07-10
中国
临床一期
2022-05-23
日本
临床一期
2021-08-11
合成路线与中间体5 routes
原研路线 × 0优化路线（非专利）× 5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 10 · 总收率 280 mg (Elinzanetant)
Elinzanetant-001212650-43-6Elinzanetant-002955401-37-3Elinzanetant-003929047-52-9Elinzanetant-004929047-53-0Elinzanetant-005929047-30-3Elinzanetant-006825643-73-0Elinzanetant-007929047-32-5Elinzanetant-0082135332-08-8Elinzanetant-0091256823-62-7Elinzanetant-010139911-29-8Elinzanetant-011825643-62-7Elinzanetant-012289686-69-7API · 依林奈坦
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Elinzanetant-001 | 212650-43-6在售 | 4-(tert-butoxycarbonyl)morpholine-3-carboxylic acid |
| Elinzanetant-002 | 955401-37-3在售 | tert-butyl 3-(((R)-3-hydroxy-1-methoxy-1-oxopropan-2-yl)carbamoyl)morpholine-4-carboxylate |
| Elinzanetant-003 | 929047-52-9在售 | (7R)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazine-6,9-dione |
| Elinzanetant-004 | 929047-53-0在售 | ((7S)-octahydropyrazino[2,1-c][1,4]oxazin-7-yl)methanol |
| Elinzanetant-005 | 929047-30-3在售 | (7S,9aS)-7-(((tert-butyldimethylsilyl)oxy)methyl)octahydropyrazino[2,1-c][1,4]oxazine |
| Elinzanetant-006 | 825643-73-0在售 | 2-(3,5-bis(trifluoromethyl)phenyl)-N-(6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl)-N,2-dimethylpropanamide |
| Elinzanetant-007 | 929047-32-5在售 | 2-(3,5-bis(trifluoromethyl)phenyl)-N-(6-((7S,9aS)-7-(((tert-butyldimethylsilyl)oxy)methyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl)-4-(4-fluoro-2-methylphenyl)pyridin-3-yl)-N,2-dimethylpropanamide |
| Elinzanetant-008 | 2135332-08-8在售 | tert-butyl (6-chloro-4-methylpyridin-3-yl)(methyl)carbamate |
| Elinzanetant-009 | 1256823-62-7在售 | 6-chloro-N,4-dimethylpyridin-3-amine |
| Elinzanetant-010 | 139911-29-8在售 | (4-fluoro-2-methylphenyl)boronic acid |
| Elinzanetant-011 | 825643-62-7在售 | 6-chloro-4-(4-fluoro-2-methylphenyl)-N-methylpyridin-3-amine |
| Elinzanetant-012 | 289686-69-7在售 | 2-(3,5-bis(trifluoromethyl)phenyl)-2-methylpropanoyl chloride |
优化Route 2步骤 8 · 总收率 /
(I)448314-1-a5350-93-6(II)448314-1-a171178-45-3(III)448314-1-a400777-00-6(IV)448314-1-a74-88-4(V)448314-1-a825643-58-1(VI)448314-1-a825643-59-2(VII)448314-1-a139911-29-8(VIII)448314-1-a825643-62-7(IX)448314-1-a289686-69-7(X)448314-1-a—(XI)448314-1-a,(XI)448314-1-b929047-30-3(XII)448314-1-a—API · 依林奈坦
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)448314-1-a | 5350-93-6在售 | 3-Amino-6-chloropyridine |
| (II)448314-1-a | 171178-45-3在售 | 1,1-Dimethylethyl (6-Chloro-3-pyridinyl)carbamate |
| (III)448314-1-a | 400777-00-6在售 | N-(6-Chloro-4-iodopyridin-3-yl)carbamic acid tert-butyl ester |
| (IV)448314-1-a | 74-88-4在售 | Iodomethane |
| (V)448314-1-a | 825643-58-1在售 | 6-Chloro-4-iodo-N-methyl-N-Boc-pyridin-3-amine |
| (VI)448314-1-a | 825643-59-2在售 | 6-Chloro-4-iodo-N-methylpyridin-3-amine |
| (VII)448314-1-a | 139911-29-8在售 | 4-Fluoro-2-methylphenylboronic acid |
| (VIII)448314-1-a | 825643-62-7在售 | 6-Chloro-4-(4-fluoro-2-methylphenyl)-N-methylpyridin-3-amine |
| (IX)448314-1-a | 289686-69-7在售 | 2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoyl chloride |
| (X)448314-1-a | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide |
| (XI)448314-1-a,(XI)448314-1-b | 929047-30-3在售 | (7S,9aS)-7-([[tert-Butyl(dimethyl)silyl]oxy]methyl)octahydropyrazino[2,1-c][1,4]oxazine |
| (XII)448314-1-a | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-[(7S,9aS)-7-([[tert-butyl(dimethyl)silyl]oxy]methyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide |
优化Route 3步骤 6 · 总收率 /
(XI)448314-1-a,(XI)448314-1-b929047-30-3(XIII)448314-1-b212650-43-6(XIV)448314-1-b5874-57-7(XIX)448314-1-b869681-70-9(XV)448314-1-b—(XVI)448314-1-b929047-27-8(XVII)448314-1-b929047-29-0(XVIII)448314-1-b131110-76-4(XX)448314-1-b—(XXI)448314-1-b—(XXII)448314-1-b—(XXIII)448314-1-b—API · 依林奈坦
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XI)448314-1-a,(XI)448314-1-b | 929047-30-3在售 | (7S,9aS)-7-([[tert-Butyl(dimethyl)silyl]oxy]methyl)octahydropyrazino[2,1-c][1,4]oxazine |
| (XIII)448314-1-b | 212650-43-6在售 | 4-[(tert-Butoxy)carbonyl]morpholine-3-carboxylic acid |
| (XIV)448314-1-b | 5874-57-7在售 | (R)-Methyl 2-amino-3-hydroxypropanoate hydrochloride |
| (XIX)448314-1-b | 869681-70-9在售 | (3R)-4-(tert-Butoxycarbonyl)morpholine-3-carboxylic acid |
| (XV)448314-1-b | - | tert-Butyl 3-[[(2R)-3-hydroxy-1-methoxy-1-oxopropan-2-yl]carbamoyl]morpholine-4-carboxylate |
| (XVI)448314-1-b | 929047-27-8在售 | (7R)-7-(Hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazine-6,9-dione |
| (XVII)448314-1-b | 929047-29-0在售 | [(7S)-Octahydropyrazino[2,1-c][1,4]oxazin-7-yl]methanol |
| (XVIII)448314-1-b | 131110-76-4在售 | N-Benzyl-D-serine methyl ester |
| (XX)448314-1-b | - | tert-Butyl (3R)-3-[benzyl[(2R)-3-hydroxy-1-methoxy-1-oxopropan-2-yl]carbamoyl]morpholine-4-carboxylate |
| (XXI)448314-1-b | - | (7R,9aR)-8-Benzyl-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazine-6,9-dione |
| (XXII)448314-1-b | - | [(7S,9aS)-8-Benzyloctahydropyrazino[2,1-c][1,4]oxazin-7-yl]methanol |
| (XXIII)448314-1-b | - | (7S,9aS)-8-Benzyl-7-([[tert-butyl(dimethyl)silyl]oxy]methyl)octahydropyrazino[2,1-c][1,4]oxazine |
优化Route 4步骤 10 · 总收率 /
(I)448314-2-a106910-77-4(II)448314-2-a79-04-9(III)448314-2-a106973-36-8(IV)448314-2-a—(V)448314-2-a218594-79-7(VI)448314-2-a47173-80-8(VII)448314-2-a—(VIII)448314-2-a—(IX)448314-2-a—(X)448314-2-a—(XI)448314-2-a—(XII)448314-2-a,(XII)448314-2-b—(XIIIa)448314-2-a—(XIIIb)448314-2-a—API · 依林奈坦
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)448314-2-a | 106910-77-4在售 | N-Benzyl-D-serine |
| (II)448314-2-a | 79-04-9在售 | 2-Chloranylethanoyl chloride |
| (III)448314-2-a | 106973-36-8在售 | 4-Benzyl-5-oxomorpholine-3(R)-carboxylic acid |
| (IV)448314-2-a | - | [(3S)-4-Benzylmorpholin-3-yl]methanol hydrogen chloride (1/1) |
| (V)448314-2-a | 218594-79-7在售 | [(3S)-Morpholin-3-yl]methanol hydrogen chloride (1/1) |
| (VI)448314-2-a | 47173-80-8在售 | 3-(Benzyloxy)-2(R)-(tert-butoxycarbonylamino)propionic acid |
| (VII)448314-2-a | - | tert-Butyl [(2R)-3-(benzyloxy)-1-[(3S)-3-(hydroxymethyl)morpholin-4-yl]-1-oxopropan-2-yl]carbamate |
| (VIII)448314-2-a | - | tert-Butyl [(2S)-1-(benzyloxy)-3-[(3S)-3-(hydroxymethyl)morpholin-4-yl]propan-2-yl]carbamate |
| (IX)448314-2-a | - | tert-Butyl [(2S)-1-(benzyloxy)-3-[(3R)-3-(chloromethyl)morpholin-4-yl]propan-2-yl]carbamate |
| (X)448314-2-a | - | (2S)-1-(Benzyloxy)-3-[(3R)-3-(chloromethyl)morpholin-4-yl]propan-2-amine |
| (XI)448314-2-a | - | (7S,9aS)-7-[(Benzyloxy)methyl]octahydropyrazino[2,1-c][1,4]oxazine |
| (XII)448314-2-a,(XII)448314-2-b | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide |
| (XIIIa)448314-2-a | - | N-[6-[(7S,9aS)-7-[(Benzyloxy)methyl]hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethylpropanamide hydrogen chloride (1/2) |
| (XIIIb)448314-2-a | - | N-[6-[(7S,9aS)-7-[(Benzyloxy)methyl]hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethylpropanamide |
优化Route 5步骤 5 · 总收率 /
(XII)448314-2-a,(XII)448314-2-b—(XIV)448314-2-b850663-54-6(XIX)448314-2-b289686-69-7(XV)448314-2-b139911-29-8(XVI)448314-2-b2642577-27-1(XVII)448314-2-b2642577-29-3(XVIII)448314-2-b—(XX)448314-2-b289686-70-0(XXI)448314-2-b—(XXII)448314-2-b74-88-4API · 依林奈坦
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XII)448314-2-a,(XII)448314-2-b | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide |
| (XIV)448314-2-b | 850663-54-6在售 | 4-Chloro-5-nitropyridin-2(1H)-one |
| (XIX)448314-2-b | 289686-69-7在售 | 2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoyl chloride |
| (XV)448314-2-b | 139911-29-8在售 | 4-Fluoro-2-methylphenylboronic acid |
| (XVI)448314-2-b | 2642577-27-1在售 | 4-(4-Fluoro-2-methylphenyl)-5-nitropyridin-2(1H)-one |
| (XVII)448314-2-b | 2642577-29-3在售 | 2-Chloro-4-(4-fluoro-2-methylphenyl)-5-nitropyridine |
| (XVIII)448314-2-b | - | 6-Chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-amine hydrogen chloride (1/1) |
| (XX)448314-2-b | 289686-70-0在售 | 2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoic acid |
| (XXI)448314-2-b | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-2-methylpropanamide |
| (XXII)448314-2-b | 74-88-4在售 | Iodomethane |
常见问题（FAQ）
依林奈坦的适应症有哪些？
已批准的适应症包括：热潮红、血管舒缩症。
依林奈坦的专利什么时候到期？
依林奈坦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。
依林奈坦有几条合成路线？
本站收录 5 条合成路线，最短路线 5 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
依林奈坦的关键中间体在哪里可以采购？
依林奈坦的多条路线中间体已挂接 CAS 档案，其中 32 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。
如何获取依林奈坦中间体的报价？
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） · 2026-10-22