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那米司特
Tier C · 观察 / 贸易Nerandomilast
勃林格殷格翰
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：PDE4B
商品名：Jascayd、博优维
适应症（已批准）：特发性肺纤维化、间质性肺疾病、肺纤维化
各地区研发/上市状态
美国
批准上市
2025-10-07
欧盟
批准上市
2026-07-15
中国
批准上市
2025-10-21
日本
批准上市
2026-05-18
合成路线与中间体3 routes
原研路线 × 0优化路线（非专利）× 3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)805433-1-a2365-48-2(II)805433-1-a96-33-3(III)805433-1-a7400-45-5(IV)805433-1-a—(V)805433-1-a57-13-6(VI)805433-1-a1196101-46-8(VII)805433-1-a913581-92-7(VIII)805433-1-a74901-69-2(IXa)805433-1-a—(IXb)805433-1-a,(IXb)805433-1-c1392213-15-8(X)805433-1-a98071-16-0(XI)805433-1-a—(XII)805433-1-a1423719-36-1(XIIIa)805433-1-a,(XIIIa)805433-1-b—(XIIIb)805433-1-a,(XIIIb)805433-1-b1423719-37-2(XIIIc)805433-1-a,(XIIIc)805433-1-b1423719-41-8(XIV)805433-1-a,(XIV)805433-1-b—(XVIIa)805433-1-b951625-94-8API · 那米司特
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)805433-1-a | 2365-48-2 | 2-Mercaptoacetic acid methyl ester |
| (II)805433-1-a | 96-33-3 | 2-Propenoic acid methyl ester |
| (III)805433-1-a | 7400-45-5 | 3-(Methoxycarbonylmethylthio)propionsauremethylester |
| (IV)805433-1-a | - | 2-Carbomethoxy-2,3,4,5-tetrahydrothiophen-3-one |
| (V)805433-1-a | 57-13-6 | Carbamide |
| (VI)805433-1-a | 1196101-46-8 | 3-Ureido-4,5-dihydro-thiophene-2-carboxylic acid methyl ester |
| (VII)805433-1-a | 913581-92-7 | 6,7-Dihydrothieno[3,2-d]pyrimidine-2,4-diol |
| (VIII)805433-1-a | 74901-69-2在售 | 2,4-Dichloro-6,7-dihydrothieno[3,2-d]pyrimidine |
| (IXa)805433-1-a | - | (1-Aminocyclobutyl)methanol tosylate |
| (IXb)805433-1-a,(IXb)805433-1-c | 1392213-15-8在售 | (1-Aminocyclobutyl)methanol hydrogen chloride |
| (X)805433-1-a | 98071-16-0 | 1-Aminocyclobutanecarboxylic acid hydrochloride |
| (XI)805433-1-a | - | [1-[(2-Chloro-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl)amino]cyclobutyl]methanol |
| (XII)805433-1-a | 1423719-36-1 | (5R)-2-Chloro-4-[[1-(hydroxymethyl)cyclobutyl]amino]-6,7-dihydro-5H-5lambda4-thieno[3,2-d]pyrimidin-5-one |
| (XIIIa)805433-1-a,(XIIIa)805433-1-b | - | 5-Chloro-2-(piperidin-4-yl)pyrimidine hydrogen chloride |
| (XIIIb)805433-1-a,(XIIIb)805433-1-b | 1423719-37-2 | 4-Methylbenzene-1-sulfonic acid 5-chloro-2-(piperidin-4-yl)pyrimidine |
| (XIIIc)805433-1-a,(XIIIc)805433-1-b | 1423719-41-8 | 5-Chloro-2-(piperidin-4-yl)pyrimidine sulfate |
| (XIV)805433-1-a,(XIV)805433-1-b | - | 4-(5-Chloropyrimidin-2-yl)piperidin-1-ium hexafluoridophosphate(1-) |
| (XVIIa)805433-1-b | 951625-94-8 | Piperidine-4-carboximidamide |
优化Route 2步骤 4 · 总收率 /
(XIIIa)805433-1-a,(XIIIa)805433-1-b—(XIIIb)805433-1-a,(XIIIb)805433-1-b1423719-37-2(XIIIc)805433-1-a,(XIIIc)805433-1-b1423719-41-8(XIV)805433-1-a,(XIV)805433-1-b—(XIX)805433-1-b5750-76-5(XV)805433-1-b4395-98-6(XVI)805433-1-b—(XVIIa)805433-1-b951625-94-8(XVIIb)805433-1-b1245647-87-3(XVIII)805433-1-b249561-98-6(XX)805433-1-b22536-67-0(XXI)805433-1-b874676-81-0(XXII)805433-1-b286961-14-6(XXIII)805433-1-b—(XXIV)805433-1-b—API · 那米司特
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XIIIa)805433-1-a,(XIIIa)805433-1-b | - | 5-Chloro-2-(piperidin-4-yl)pyrimidine hydrogen chloride |
| (XIIIb)805433-1-a,(XIIIb)805433-1-b | 1423719-37-2 | 4-Methylbenzene-1-sulfonic acid 5-chloro-2-(piperidin-4-yl)pyrimidine |
| (XIIIc)805433-1-a,(XIIIc)805433-1-b | 1423719-41-8 | 5-Chloro-2-(piperidin-4-yl)pyrimidine sulfate |
| (XIV)805433-1-a,(XIV)805433-1-b | - | 4-(5-Chloropyrimidin-2-yl)piperidin-1-ium hexafluoridophosphate(1-) |
| (XIX)805433-1-b | 5750-76-5 | 2,4,5-Trichloropyrimidine |
| (XV)805433-1-b | 4395-98-6 | 4-Piperidinecarbonitrile |
| (XVI)805433-1-b | - | Methyl piperidine-4-carboximidate hydrogen chloride |
| (XVIIa)805433-1-b | 951625-94-8 | Piperidine-4-carboximidamide |
| (XVIIb)805433-1-b | 1245647-87-3 | Piperidine-4-carboximidamide hydrogen chloride |
| (XVIII)805433-1-b | 249561-98-6 | 2-Chloro-1,3-bis(dimentylamino)trimethinium hexafluorophosphate |
| (XX)805433-1-b | 22536-67-0 | 2,5-Dichloropyrimidine |
| (XXI)805433-1-b | 874676-81-0 | 5-Chloro-2-iodopyrimidine |
| (XXII)805433-1-b | 286961-14-6 | (1-tert-Butoxycarbonyl-1,2,3,6-tetrahydropyridin-4-yl)boronic acid pinacol ester |
| (XXIII)805433-1-b | - | Boc-4-(5-chloropyrimidin-2-yl)-3,6-dihydropyridine |
| (XXIV)805433-1-b | - | Boc-4-(5-chloropyrimidin-2-yl)piperidine |
优化Route 3步骤 3 · 总收率 /
(IXb)805433-1-a,(IXb)805433-1-c1392213-15-8(XIIIc)805433-1-a,(XIIIc)805433-1-b1423719-41-8(XXV)805433-1-c120728-10-1(XXVI)805433-1-c—(XXVII)805433-1-c1142211-17-3API · 那米司特
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (IXb)805433-1-a,(IXb)805433-1-c | 1392213-15-8在售 | (1-Aminocyclobutyl)methanol hydrogen chloride |
| (XIIIc)805433-1-a,(XIIIc)805433-1-b | 1423719-41-8 | 5-Chloro-2-(piperidin-4-yl)pyrimidine sulfate |
| (XXV)805433-1-c | 120728-10-1在售 | 1-((1,1-Dimethylethoxycarbonyl)amino)cyclobutanecarboxylic acid |
| (XXVI)805433-1-c | - | Methyl 1-(Boc-amino)cyclobutanecarboxylate |
| (XXVII)805433-1-c | 1142211-17-3 | 1-(Boc-amino)-1-(hydroxymethyl)cyclobutane |
常见问题（FAQ）
那米司特的适应症有哪些？
已批准的适应症包括：特发性肺纤维化、间质性肺疾病、肺纤维化。
那米司特的专利什么时候到期？
那米司特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。
那米司特有几条合成路线？
本站收录 3 条合成路线，最短路线 3 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
那米司特的关键中间体在哪里可以采购？
那米司特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。
如何获取那米司特中间体的报价？
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