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Cipargamin
Tier C · 观察 / 贸易Cipargamin
诺华制药
原研
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首批上市
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到期年（公开口径）
无销量数据
峰值销售
化学药
类型
靶点：PfATP4
适应症（已批准）：恶性疟、疟原虫感染
各地区研发/上市状态
美国
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欧盟
无进展
2020-07-22
中国
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日本
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合成路线与中间体4 routes
原研路线 × 1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。
原研Route 1步骤 13 · 总收率 10.8 g
CIPARG-00117630-76-1CIPARG-002879563-65-2CIPARG-00317366-80-2CIPARG-0041809076-21-8CIPARG-0051809076-20-7CIPARG-0061809076-22-9CIPARG-0071809076-23-0CIPARG-0081809076-24-1CIPARG-0091809076-25-2CIPARG-0101809076-26-3CIPARG-0111809076-27-4CIPARG-0121809076-28-5CIPARG-0131809076-29-6CIPARG-0141809076-30-9CIPARG-015143101-26-2Cipargamin1193314-23-6API · Cipargamin
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CIPARG-001 | 17630-76-1 | 5-chloroindoline-2,3-dione |
| CIPARG-002 | 879563-65-2 | 5-chloro-1-(4-methoxybenzyl)indoline-2,3-dione |
| CIPARG-003 | 17366-80-2 | P,P-diphenylphosphinothioic amide |
| CIPARG-004 | 1809076-21-8 | (E)-N-(5-chloro-1-(4-methoxybenzyl)-2-oxoindolin-3-ylidene)-P,P-diphenylphosphinothioic amide |
| CIPARG-005 | 1809076-20-7 | tert-butyl (5-chloro-2-ethynyl-4-fluorophenyl)carbamate |
| CIPARG-006 | 1809076-22-9 | tert-butyl (S)-(5-chloro-2-((5-chloro-3-((diphenylphosphorothioyl)amino)-1-(4-methoxybenzyl)-2-oxoindolin-3-yl)ethynyl)-4-fluorophenyl)carbamate |
| CIPARG-007 | 1809076-23-0 | (S)-N-(3-((2-amino-4-chloro-5-fluorophenyl)ethynyl)-5-chloro-1-(4-methoxybenzyl)-2-oxoindolin-3-yl)-P,P-diphenylphosphinothioic amide |
| CIPARG-008 | 1809076-24-1 | (R)-N-(5-chloro-3-(6-chloro-5-fluoro-1H-indol-2-yl)-1-(4-methoxybenzyl)-2-oxoindolin-3-yl)-P,P-diphenylphosphinothioic amide |
| CIPARG-009 | 1809076-25-2 | (R)-3-amino-5-chloro-3-(6-chloro-5-fluoro-1H-indol-2-yl)-1-(4-methoxybenzyl)indolin-2-one |
| CIPARG-010 | 1809076-26-3 | benzyl (R)-(5-chloro-3-(6-chloro-5-fluoro-1H-indol-2-yl)-1-(4-methoxybenzyl)-2-oxoindolin-3-yl)carbamate |
| CIPARG-011 | 1809076-27-4 | benzyl (R)-(5-chloro-3-(6-chloro-5-fluoro-3-formyl-1H-indol-2-yl)-1-(4-methoxybenzyl)-2-oxoindolin-3-yl)carbamate |
| CIPARG-012 | 1809076-28-5 | benzyl (R,E)-(5-chloro-3-(6-chloro-5-fluoro-3-(2-nitroprop-1-en-1-yl)-1H-indol-2-yl)-1-(4-methoxybenzyl)-2-oxoindolin-3-yl)carbamate |
| CIPARG-013 | 1809076-29-6 | benzyl (R)-(5-chloro-3-(6-chloro-5-fluoro-3-(2-oxopropyl)-1H-indol-2-yl)-1-(4-methoxybenzyl)-2-oxoindolin-3-yl)carbamate |
| CIPARG-014 | 1809076-30-9 | (3R,3'S)-5,7'-dichloro-6'-fluoro-1-(4-methoxybenzyl)-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3,4-b]indol]-2-one |
| CIPARG-015 | 143101-26-2 | 5-chloro-2-ethynyl-4-fluoroaniline |
| Cipargamin | 1193314-23-6 | (3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3,4-b]indol]-2-one |
优化Route 2步骤 10 · 总收率 15 mg
CIPARG-020—CIPARG-0211193314-78-1CIPARG-0221193314-79-2CIPARG-0231193314-80-5CIPARG-0241193314-81-6CIPARG-0251193314-86-1Cipargamin1193314-23-6CIPARG-00117630-76-1CIPARG-016122509-72-2CIPARG-0171193314-76-9CIPARG-0181193314-77-0CIPARG-0192007920-27-4API · Cipargamin
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CIPARG-020 | - | methyl (R)-2-amino-3-(6-chloro-5-fluoro-1H-indol-3-yl)propanoate |
| CIPARG-021 | 1193314-78-1 | methyl (R)-2-((tert-butoxycarbonyl)amino)-3-(6-chloro-5-fluoro-1H-indol-3-yl)propanoate |
| CIPARG-022 | 1193314-79-2 | tert-butyl (R)-(1-(6-chloro-5-fluoro-1H-indol-3-yl)-3-hydroxypropan-2-yl)carbamate |
| CIPARG-023 | 1193314-80-5 | (R)-2-((tert-butoxycarbonyl)amino)-3-(6-chloro-5-fluoro-1H-indol-3-yl)propyl methanesulfonate |
| CIPARG-024 | 1193314-81-6 | tert-butyl (S)-(1-(6-chloro-5-fluoro-1H-indol-3-yl)propan-2-yl)carbamate |
| CIPARG-025 | 1193314-86-1 | (S)-1-(6-chloro-5-fluoro-1H-indol-3-yl)propan-2-amine |
| Cipargamin | 1193314-23-6 | (3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3,4-b]indol]-2-one |
| CIPARG-001 | 17630-76-1 | 5-chloroindoline-2,3-dione |
| CIPARG-016 | 122509-72-2 | 6-chloro-5-fluoro-1H-indole |
| CIPARG-017 | 1193314-76-9 | 2-acetamido-3-(6-chloro-5-fluoro-1H-indol-3-yl)propanoic acid |
| CIPARG-018 | 1193314-77-0 | (R)-2-acetamido-3-(6-chloro-5-fluoro-1H-indol-3-yl)propanoic acid |
| CIPARG-019 | 2007920-27-4 | (R)-2-amino-3-(6-chloro-5-fluoro-1H-indol-3-yl)propanoic acid |
优化Route 3步骤 6 · 总收率 26.23 g
CIPARG-00117630-76-1CIPARG-02696202-57-2CIPARG-0271458665-06-9CIPARG-0281458665-07-0CIPARG-0291458665-08-1CIPARG-030—CIPARG-031—Cipargamin1193314-23-6API · Cipargamin
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CIPARG-001 | 17630-76-1 | 5-chloroindoline-2,3-dione |
| CIPARG-026 | 96202-57-2 | 6-chloro-5-fluoroindoline-2,3-dione |
| CIPARG-027 | 1458665-06-9 | 6-chloro-5-fluoro-3-hydroxy-3-(2-oxopropyl)indolin-2-one |
| CIPARG-028 | 1458665-07-0 | 6-chloro-5-fluoro-3-hydroxy-3-((2-methyl-1,3-dioxolan-2-yl)methyl)indolin-2-one |
| CIPARG-029 | 1458665-08-1 | 1-(6-chloro-5-fluoro-1H-indol-3-yl)propan-2-one |
| CIPARG-030 | - | (S)-1-(6-chloro-5-fluoro-1H-indol-3-yl)propan-2-amine (7,7-dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid |
| CIPARG-031 | - | (3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3,4-b]indol]-2-one (7,7-dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid |
| Cipargamin | 1193314-23-6 | (3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3,4-b]indol]-2-one |
优化Route 4步骤 5 · 总收率 /
CIPARG-00117630-76-1CIPARG-016122509-72-2CIPARG-032467451-99-6CIPARG-0331458665-11-6CIPARG-0341193314-75-8CIPARG-0351193314-69-0Cipargamin1193314-23-6API · Cipargamin
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CIPARG-001 | 17630-76-1 | 5-chloroindoline-2,3-dione |
| CIPARG-016 | 122509-72-2 | 6-chloro-5-fluoro-1H-indole |
| CIPARG-032 | 467451-99-6 | 6-chloro-5-fluoro-1H-indole-3-carbaldehyde |
| CIPARG-033 | 1458665-11-6 | (Z)-6-chloro-5-fluoro-3-(2-nitroprop-1-en-1-yl)-1H-indole |
| CIPARG-034 | 1193314-75-8 | 1-(6-chloro-5-fluoro-1H-indol-3-yl)propan-2-amine |
| CIPARG-035 | 1193314-69-0 | 5,7'-dichloro-6'-fluoro-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3,4-b]indol]-2-one |
| Cipargamin | 1193314-23-6 | (3R,3'S)-5,7'-dichloro-6'-fluoro-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3,4-b]indol]-2-one |
常见问题（FAQ）
Cipargamin的适应症有哪些？
已批准的适应症包括：恶性疟、疟原虫感染。
Cipargamin的专利什么时候到期？
Cipargamin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。
Cipargamin有几条合成路线？
本站收录 4 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。
Cipargamin的关键中间体在哪里可以采购？
Cipargamin路线中的中间体均已建立 CAS 档案，可直接按 CAS 发起询价，需求会进入供应网络撮合池。
如何获取Cipargamin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） · 2026-10-18