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依替巴肽
Tier C · 观察 / 贸易Eptifibatide
Millennium Pharmaceuticals Inc
原研
1998
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：GP IIb/IIIa
商品名：Integrilin、Integrelin (former Brand Name)
适应症（已批准）：不稳定型心绞痛、心肌梗塞
各地区研发/上市状态
美国
撤市
欧盟
撤市
中国
批准上市
2012-10-30
日本
-
合成路线与中间体5 routes
原研路线 × 1优化路线（非专利）× 4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 8 · 总收率 /
EPTI-014953424-19-6EPTI-01522906-75-8EPTI-001103213-32-7EPTI-002—EPTI-00371989-31-6EPTI-004—EPTI-005143824-78-6EPTI-006—EPTI-008—EPTI-00929022-11-5EPTI-010—EPTI-01171989-26-9EPTI-00771989-14-5EPTI-012—EPTI-01327144-18-9API · 依替巴肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPTI-014 | 953424-19-6 | (7S,13S)-tert-butyl 13-(((S)-1-((S)-2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)carbamoyl)-7-(4-aminobutyl)-5,8,11-trioxo-1,1,1-triphenyl-2-thia-6,9,12-triazapentadecan-15-oate |
| EPTI-015 | 22906-75-8 | 3,5-dimethyl-1H-pyrazole-1-carboximidamide |
| EPTI-001 | 103213-32-7 | N-(((9H-fluoren-9-yl)methoxy)carbonyl)-S-trityl-L-cysteine |
| EPTI-002 | - | (9H-fluoren-9-yl)methyl (R)-(1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamate |
| EPTI-003 | 71989-31-6 | (((9H-fluoren-9-yl)methoxy)carbonyl)-L-proline |
| EPTI-004 | - | (9H-fluoren-9-yl)methyl (S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidine-1-carboxylate |
| EPTI-005 | 143824-78-6 | Na-(((9H-fluoren-9-yl)methoxy)carbonyl)-1-(tert-butoxycarbonyl)-L-tryptophan |
| EPTI-006 | - | (9H-fluoren-9-yl)methyl ((S)-3-(1H-indol-3-yl)-1-((S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxopropan-2-yl)carbamate |
| EPTI-008 | - | (S)-tert-butyl 4-(((S)-3-(1H-indol-3-yl)-1-((S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxopropan-2-yl)amino)-3-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-oxobutanoate |
| EPTI-009 | 29022-11-5 | (((9H-fluoren-9-yl)methoxy)carbonyl)glycine |
| EPTI-010 | - | (S)-tert-butyl 4-(((S)-3-(1H-indol-3-yl)-1-((S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxopropan-2-yl)amino)-3-(2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)acetamido)-4-oxobutanoate |
| EPTI-011 | 71989-26-9 | (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-6-((tert-butoxycarbonyl)amino)hexanoic acid |
| EPTI-007 | 71989-14-5 | (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-(tert-butoxy)-4-oxobutanoic acid |
| EPTI-012 | - | (10S,16S)-tert-butyl 16-(((S)-3-(1H-indol-3-yl)-1-((S)-2-(((R)-1-(methylamino)-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-oxopropan-2-yl)carbamoyl)-10-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-2,2-dimethyl-4,11,14-trioxo-3-oxa-5,12,15-triazaoctadecan-18-oate |
| EPTI-013 | 27144-18-9 | 3-(tritylthio)propanoic acid |
优化Route 2步骤 8 · 总收率 1.20 g
EPTI-01656-40-6EPTI-0175680-79-5EPTI-0181313054-55-5EPTI-0191333244-82-8EPTI-02052574-08-0EPTI-0211234363-80-4EPTI-0221416568-03-0EPTI-0231416568-06-3EPTI-02488530-32-9EPTI-025147-85-3EPTI-0262133-40-6EPTI-0277432-21-5EPTI-028107312-97-0EPTI-0295545-52-8API · 依替巴肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPTI-016 | 56-40-6在售 | 2-aminoacetic acid |
| EPTI-017 | 5680-79-5在售 | methyl glycinate hydrochloride |
| EPTI-018 | 1313054-55-5 | (S)-2-(((benzyloxy)carbonyl)amino)-6-guanidinohexanoic acid |
| EPTI-019 | 1333244-82-8 | (S)-methyl 2-(2-amino-6-guanidinohexanamido)acetate |
| EPTI-020 | 52574-08-0 | 3-((acetamidomethyl)thio)propanoic acid |
| EPTI-021 | 1234363-80-4 | (S)-10-(4-guanidinobutyl)-2,8,11-trioxo-5-thia-3,9,12-triazatetradecan-14-oic acid |
| EPTI-022 | 1416568-03-0 | (S)-methyl 1-((S)-2-((S)-2-amino-4-(tert-butoxy)-4-oxobutanamido)-3-(1H-indol-3-yl)propanoyl)pyrrolidine-2-carboxylate |
| EPTI-023 | 1416568-06-3 | (S)-1-((10S,16S,19S)-19-((1H-indol-3-yl)methyl)-16-(2-(tert-butoxy)-2-oxoethyl)-10-(4-guanidinobutyl)-2,8,11,14,17-pentaoxo-5-thia-3,9,12,15,18-pentaazaicosan-20-oyl)pyrrolidine-2-carboxylic acid |
| EPTI-024 | 88530-32-9 | (R)-3-((acetamidomethyl)thio)-2-aminopropanamide |
| EPTI-025 | 147-85-3 | (S)-pyrrolidine-2-carboxylic acid |
| EPTI-026 | 2133-40-6 | methyl L-prolinate hydrochloride |
| EPTI-027 | 7432-21-5 | (S)-2-(((benzyloxy)carbonyl)amino)-3-(1H-indol-3-yl)propanoic acid |
| EPTI-028 | 107312-97-0 | (S)-methyl 1-((S)-2-amino-3-(1H-indol-3-yl)propanoyl)pyrrolidine-2-carboxylate |
| EPTI-029 | 5545-52-8 | (S)-2-(((benzyloxy)carbonyl)amino)-4-(tert-butoxy)-4-oxobutanoic acid |
优化Route 3步骤 9 · 总收率 /
EPTI-00371989-31-6EPTI-00771989-14-5EPTI-01327144-18-9EPTI-0175680-79-5EPTI-0302389-60-8EPTI-03110342-52-6EPTI-0321423453-42-2EPTI-0331418304-71-8EPTI-0341423453-48-8EPTI-0351423453-54-6EPTI-036380600-10-2EPTI-037166737-85-5EPTI-0381423453-22-8EPTI-03935737-15-6EPTI-0401423453-28-4EPTI-0411423453-33-1API · 依替巴肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPTI-003 | 71989-31-6 | (((9H-fluoren-9-yl)methoxy)carbonyl)-L-proline |
| EPTI-007 | 71989-14-5 | (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-(tert-butoxy)-4-oxobutanoic acid |
| EPTI-013 | 27144-18-9 | 3-(tritylthio)propanoic acid |
| EPTI-017 | 5680-79-5在售 | methyl glycinate hydrochloride |
| EPTI-030 | 2389-60-8 | (S)-2-(((benzyloxy)carbonyl)amino)-6-((tert-butoxycarbonyl)amino)hexanoic acid |
| EPTI-031 | 10342-52-6 | (S)-methyl 2-(2-(((benzyloxy)carbonyl)amino)-6-((tert-butoxycarbonyl)amino)hexanamido)acetate |
| EPTI-032 | 1423453-42-2 | (S)-methyl 2-(6-((tert-butoxycarbonyl)amino)-2-(3-(tritylthio)propanamido)hexanamido)acetate |
| EPTI-033 | 1418304-71-8 | (S)-tert-butyl 3-amino-4-(((S)-1-((S)-2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-4-oxobutanoate |
| EPTI-034 | 1423453-48-8 | (10S,16S)-tert-butyl 16-(((S)-1-((S)-2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)carbamoyl)-2,2-dimethyl-4,11,14-trioxo-10-(3-(tritylthio)propanamido)-3-oxa-5,12,15-triazaoctadecan-18-oate |
| EPTI-035 | 1423453-54-6 | 2-((3R,11S,17S,20S,25aS)-20-((1H-indol-3-yl)methyl)-11-(4-aminobutyl)-3-carbamoyl-1,9,12,15,18,21-hexaoxodocosahydro-1H-pyrrolo[2,1-g][1,2,5,8,11,14,17,20]dithiahexaazacyclotricosin-17-yl)acetic acid hydrochloride |
| EPTI-036 | 380600-10-2 | amino(imino)methanesulfonic acid hydrate |
| EPTI-037 | 166737-85-5 | (R)-2-amino-3-(tritylthio)propanamide |
| EPTI-038 | 1423453-22-8 | (S)-(9H-fluoren-9-yl)methyl 2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidine-1-carboxylate |
| EPTI-039 | 35737-15-6 | (((9H-fluoren-9-yl)methoxy)carbonyl)-L-tryptophan |
| EPTI-040 | 1423453-28-4 | (9H-fluoren-9-yl)methyl ((S)-1-((S)-2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)carbamate |
| EPTI-041 | 1423453-33-1 | (S)-tert-butyl 3-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-(((S)-1-((S)-2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-4-oxobutanoate |
优化Route 4步骤 6 · 总收率 157 g
EPTI-0423338-32-7EPTI-04338136-75-3EPTI-044868242-17-5EPTI-045868242-18-6EPTI-046868242-19-7EPTI-047677729-17-8EPTI-048—EPTI-049—EPTI-050107-96-0EPTI-051868242-21-1API · 依替巴肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPTI-042 | 3338-32-7 | (S)-4-tert-butyl 1-(2,5-dioxopyrrolidin-1-yl) 2-(((benzyloxy)carbonyl)amino)succinate |
| EPTI-043 | 38136-75-3 | (S)-1-((S)-2-amino-3-(1H-indol-3-yl)propanoyl)pyrrolidine-2-carboxylic acid |
| EPTI-044 | 868242-17-5 | (S)-1-((S)-2-((S)-2-(((benzyloxy)carbonyl)amino)-4-(tert-butoxy)-4-oxobutanamido)-3-(1H-indol-3-yl)propanoyl)pyrrolidine-2-carboxylic acid |
| EPTI-045 | 868242-18-6 | (S)-1-((S)-2-((S)-2-amino-4-(tert-butoxy)-4-oxobutanamido)-3-(1H-indol-3-yl)propanoyl)pyrrolidine-2-carboxylic acid |
| EPTI-046 | 868242-19-7 | (S)-2-(2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-6-guanidinohexanamido)acetic acid |
| EPTI-047 | 677729-17-8 | (S)-1-((5S,11S,14S)-14-((1H-indol-3-yl)methyl)-11-(2-(tert-butoxy)-2-oxoethyl)-1-(9H-fluoren-9-yl)-5-(4-guanidinobutyl)-3,6,9,12-tetraoxo-2-oxa-4,7,10,13-tetraazapentadecan-15-oyl)pyrrolidine-2-carboxylic acid |
| EPTI-048 | - | (R)-2-amino-3-((3-nitropyridin-2-yl)disulfanyl)propanamide hydrochloride |
| EPTI-049 | - | (5S,11S)-tert-butyl 11-(((S)-1-((S)-2-(((R)-1-amino-3-((3-nitropyridin-2-yl)disulfanyl)-1-oxopropan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)carbamoyl)-1-(9H-fluoren-9-yl)-5-(4-guanidinobutyl)-3,6,9-trioxo-2-oxa-4,7,10-triazatridecan-13-oate |
| EPTI-050 | 107-96-0 | 3-mercaptopropanoic acid |
| EPTI-051 | 868242-21-1 | 3-(((R)-2-((S)-1-((5S,11S,14S)-14-((1H-indol-3-yl)methyl)-11-(2-(tert-butoxy)-2-oxoethyl)-1-(9H-fluoren-9-yl)-5-(4-guanidinobutyl)-3,6,9,12-tetraoxo-2-oxa-4,7,10,13-tetraazapentadecan-15-oyl)pyrrolidine-2-carboxamido)-3-amino-3-oxopropyl)disulfanyl)propanoic acid |
优化Route 5步骤 6 · 总收率 /
EPTI-001103213-32-7EPTI-00771989-14-5EPTI-01327144-18-9EPTI-025147-85-3EPTI-0411423453-33-1EPTI-0521119-34-2EPTI-053202752-01-0EPTI-05487-69-4EPTI-0551430201-39-0EPTI-056—EPTI-057—EPTI-058—EPTI-05973-22-3EPTI-06013139-14-5EPTI-061106-95-6EPTI-062—EPTI-063—EPTI-064—EPTI-065—EPTI-066—EPTI-067—API · 依替巴肽
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPTI-001 | 103213-32-7 | N-(((9H-fluoren-9-yl)methoxy)carbonyl)-S-trityl-L-cysteine |
| EPTI-007 | 71989-14-5 | (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-(tert-butoxy)-4-oxobutanoic acid |
| EPTI-013 | 27144-18-9 | 3-(tritylthio)propanoic acid |
| EPTI-025 | 147-85-3 | (S)-pyrrolidine-2-carboxylic acid |
| EPTI-041 | 1423453-33-1 | (S)-tert-butyl 3-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-(((S)-1-((S)-2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-4-oxobutanoate |
| EPTI-052 | 1119-34-2 | L-cysteine hydrochloride |
| EPTI-053 | 202752-01-0 | (R)-(9H-fluoren-9-yl)methyl (1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamate |
| EPTI-054 | 87-69-4 | (2R,3R)-2,3-dihydroxysuccinic acid |
| EPTI-055 | 1430201-39-0 | (R)-2-amino-3-(tritylthio)propanamide (2R,3R)-2,3-dihydroxysuccinate |
| EPTI-056 | - | (R)-1-((S)-2-((S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-(tert-butoxy)-4-oxobutanamido)-3-(1H-indol-3-yl)propanoyl)pyrrolidine-2-carboxylic acid |
| EPTI-057 | - | - |
| EPTI-058 | - | - |
| EPTI-059 | 73-22-3 | (S)-2-amino-3-(1H-indol-3-yl)propanoic acid |
| EPTI-060 | 13139-14-5 | (S)-2-((tert-butoxycarbonyl)amino)-3-(1H-indol-3-yl)propanoic acid |
| EPTI-061 | 106-95-6在售 | 3-bromoprop-1-ene |
| EPTI-062 | - | (R)-2-allyl 1-tert-butyl pyrrolidine-1,2-dicarboxylate |
| EPTI-063 | - | (R)-allyl 1-((S)-2-((tert-butoxycarbonyl)amino)-3-(1H-indol-3-yl)propanoyl)pyrrolidine-2-carboxylate |
| EPTI-064 | - | (R)-allyl 1-((S)-2-((S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-4-(tert-butoxy)-4-oxobutanamido)-3-(1H-indol-3-yl)propanoyl)pyrrolidine-2-carboxylate |
| EPTI-065 | - | - |
| EPTI-066 | - | - |
| EPTI-067 | - | - |
常见问题（FAQ）
依替巴肽的适应症有哪些？
已批准的适应症包括：不稳定型心绞痛、心肌梗塞。
依替巴肽的专利什么时候到期？
依替巴肽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。
依替巴肽有几条合成路线？
本站收录 5 条合成路线，最短路线 6 步、总收率 157 g。每条路线的中间体均带登记编号与 CAS 号。
依替巴肽的关键中间体在哪里可以采购？
依替巴肽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。
如何获取依替巴肽中间体的报价？
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