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Grazoprevir Hydrate
Tier C · 观察 / 贸易Grazoprevir Hydrate
默沙东
原研
2016
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：NS3/NS4A
商品名：Grazyna
适应症（已批准）：丙型肝炎
各地区研发/上市状态
美国
-
欧盟
无进展
2016-06-01
中国
临床一期
2013-11-19
日本
批准上市
2016-09-28
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 18 · 总收率 393 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| GRAZ-001 | 59548-39-9 | 4-methoxybenzene-1,2-diamine dihydrochloride |
| GRAZ-002 | 95-92-1 | diethyl oxalate |
| GRAZ-003 | 31910-18-6 | 6-methoxyquinoxaline-2,3-diol |
| GRAZ-004 | 1263814-66-9 | 3-chloro-7-methoxyquinoxalin-2-ol |
| GRAZ-005 | 438452-29-0 | (2S,4S)-1-tert-butyl 2-methyl 4-(((4-bromophenyl)sulfonyl)oxy)pyrrolidine-1,2-dicarboxylate |
| GRAZ-006 | 1206524-79-9 | 1-(tert-butyl) 2-methyl (2S,4R)-4-((3-chloro-7-methoxyquinoxalin-2-yl)oxy)pyrrolidine-1,2-dicarboxylate |
| GRAZ-007 | 1361028-94-5 | methyl (2S,4R)-4-((3-chloro-7-methoxyquinoxalin-2-yl)oxy)pyrrolidine-2-carboxylate hydrochloride |
| GRAZ-008 | 1026200-27-0 | (R)-3,3-dimethyl-2-((((1R,2R)-2-(pent-4-en-1-yl)cyclopropoxy)carbonyl)amino)butanoic acid |
| GRAZ-009 | 1206524-81-3 | methyl (2S,4R)-4-((3-chloro-7-methoxyquinoxalin-2-yl)oxy)-1-((S)-3,3-dimethyl-2-((((1R,2R)-2-(pent-4-en-1-yl)cyclopropoxy)carbonyl)amino)butanoyl)pyrrolidine-2-carboxylate |
| GRAZ-010 | 13682-77-4在售 | potassium trifluoro(vinyl)borate |
| GRAZ-011 | 1206524-82-4 | methyl (2S,4R)-1-((S)-3,3-dimethyl-2-((((1R,2R)-2-(pent-4-en-1-yl)cyclopropoxy)carbonyl)amino)butanoyl)-4-((7-methoxy-3-vinylquinoxalin-2-yl)oxy)pyrrolidine-2-carboxylate |
| GRAZ-012 | 918870-76-5 | - |
| GRAZ-013 | 1206524-83-5 | methyl (33R,35S,91R,92R,5S,E)-5-(tert-butyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphan-13-ene-35-carboxylate |
| GRAZ-014 | 1206524-84-6 | methyl (33R,35S,91R,92R,5S)-5-(tert-butyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxylate |
| GRAZ-015 | 1206524-85-7 | (33R,35S,91R,92R,5S)-5-(tert-butyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxylic acid |
| GRAZ-016 | - | (1R,2S)-1-amino-N-(cyclopropylsulfonyl)-2-vinylcyclopropanecarboxamide hydrochloride |
| GRAZ-017 | 1350514-68-9 | (33R,35S,91R,92R,5S)-5-(tert-butyl)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxamide |
| GRAZ-018 | 7103-09-5 | but-3-en-1-ylmagnesium bromide |
| GRAZ-019 | 107-02-8 | acrylaldehyde |
| GRAZ-020 | 124471-63-2 | (E)-(hepta-1,6-dien-1-yloxy)trimethylsilane |
| GRAZ-021 | - | trimethyl(2-(pent-4-en-1-yl)cyclopropoxy)silane |
| GRAZ-022 | 1823376-86-8 | 2-(pent-4-en-1-yl)cyclopropan-1-ol |
| GRAZ-023 | 1384277-03-5 | (1R,2R)-2-(pent-4-en-1-yl)cyclopropyl acetate |
| GRAZ-024 | 1206524-77-7 | (1R,2R)-2-(pent-4-en-1-yl)cyclopropan-1-ol |
| GRAZ-025 | 144164-32-9 | methyl (S)-2-isocyanato-3,3-dimethylbutanoate |
| GRAZ-026 | 1026200-25-8 | methyl (S)-3,3-dimethyl-2-((((1R,2R)-2-(pent-4-en-1-yl)cyclopropoxy)carbonyl)amino)butanoate |
优化Route 2步骤 6 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| GRAZ-006 | 1206524-79-9 | 1-(tert-butyl) 2-methyl (2S,4R)-4-((3-chloro-7-methoxyquinoxalin-2-yl)oxy)pyrrolidine-1,2-dicarboxylate |
| GRAZ-014 | 1206524-84-6 | methyl (33R,35S,91R,92R,5S)-5-(tert-butyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxylate |
| GRAZ-015 | 1206524-85-7 | (33R,35S,91R,92R,5S)-5-(tert-butyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxylic acid |
| GRAZ-027 | 1350619-77-0 | (1R,2R)-2-(pent-2-yn-1-yl)cyclopropan-1-ol |
| GRAZ-028 | 20859-02-3 | (S)-2-amino-3,3-dimethylbutanoic acid |
| GRAZ-029 | 1425038-19-2 | (R)-3,3-dimethyl-2-((((1R,2R)-2-(pent-2-yn-1-yl)cyclopropoxy)carbonyl)amino)butanoic acid |
| GRAZ-030 | 1425704-74-0 | (S)-2-((((1R,2R)-2-(5-(3-(((3R,5S)-1-(tert-butoxycarbonyl)-5-(methoxycarbonyl)pyrrolidin-3-yl)oxy)-6-methoxyquinoxalin-2-yl)pent-4-yn-1-yl)cyclopropoxy)carbonyl)amino)-3,3-dimethylbutanoic acid |
| GRAZ-031 | 1425704-76-2 | (S)-2-((((1R,2R)-2-(5-(3-(((3R,5S)-1-(tert-butoxycarbonyl)-5-(methoxycarbonyl)pyrrolidin-3-yl)oxy)-6-methoxyquinoxalin-2-yl)pentyl)cyclopropoxy)carbonyl)amino)-3,3-dimethylbutanoic acid |
| GRAZ-032 | 1028252-16-5 | (1R,2S)-1-amino-N-(cyclopropylsulfonyl)-2-vinylcyclopropane-1-carboxamide |
优化Route 3步骤 10 · 总收率 694 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| GRAZ-002 | 95-92-1 | diethyl oxalate |
| GRAZ-013 | 1206524-83-5 | methyl (33R,35S,91R,92R,5S,E)-5-(tert-butyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphan-13-ene-35-carboxylate |
| GRAZ-014 | 1206524-84-6 | methyl (33R,35S,91R,92R,5S)-5-(tert-butyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxylate |
| GRAZ-018 | 7103-09-5 | but-3-en-1-ylmagnesium bromide |
| GRAZ-027 | 1350619-77-0 | (1R,2R)-2-(pent-2-yn-1-yl)cyclopropan-1-ol |
| GRAZ-029 | 1425038-19-2 | (R)-3,3-dimethyl-2-((((1R,2R)-2-(pent-2-yn-1-yl)cyclopropoxy)carbonyl)amino)butanoic acid |
| GRAZ-033 | 102337-17-7 | ethyl 2-oxohex-5-enoate |
| GRAZ-034 | 102-51-2 | 4-methoxybenzene-1,2-diamine |
| GRAZ-035 | 1799940-44-5 | 3-(but-3-en-1-yl)-7-methoxyquinoxalin-2-ol |
| GRAZ-036 | 1799940-45-6 | 2-(but-3-en-1-yl)-3-chloro-6-methoxyquinoxaline |
| GRAZ-037 | 74844-91-0 | 1-(tert-butyl) 2-methyl (2S,4R)-4-hydroxypyrrolidine-1,2-dicarboxylate |
| GRAZ-038 | 1026204-22-7 | 1-(tert-butyl) 2-methyl (2S,4R)-4-((3-(but-3-en-1-yl)-7-methoxyquinoxalin-2-yl)oxy)pyrrolidine-1,2-dicarboxylate |
| GRAZ-039 | 1799940-46-7 | methyl (2S,4R)-4-((3-(but-3-en-1-yl)-7-methoxyquinoxalin-2-yl)oxy)pyrrolidine-2-carboxylate |
| GRAZ-040 | 1799940-51-4 | (S)-3,3-dimethyl-2-((((1R,2R)-2-((Z)-pent-2-en-1-yl)cyclopropoxy)carbonyl)amino)butanoic acid |
| GRAZ-041 | 1799940-52-5 | methyl (2S,4R)-4-((3-(but-3-en-1-yl)-7-methoxyquinoxalin-2-yl)oxy)-1-((S)-3,3-dimethyl-2-((((1R,2R)-2-((Z)-pent-2-en-1-yl)cyclopropoxy)carbonyl)amino)butanoyl)pyrrolidine-2-carboxylate |
| GRAZ-042 | 301224-40-8 | - |
优化Route 4步骤 4 · 总收率 60 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| GRAZ-008 | 1026200-27-0 | (R)-3,3-dimethyl-2-((((1R,2R)-2-(pent-4-en-1-yl)cyclopropoxy)carbonyl)amino)butanoic acid |
| GRAZ-009 | 1206524-81-3 | methyl (2S,4R)-4-((3-chloro-7-methoxyquinoxalin-2-yl)oxy)-1-((S)-3,3-dimethyl-2-((((1R,2R)-2-(pent-4-en-1-yl)cyclopropoxy)carbonyl)amino)butanoyl)pyrrolidine-2-carboxylate |
| GRAZ-013 | 1206524-83-5 | methyl (33R,35S,91R,92R,5S,E)-5-(tert-butyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphan-13-ene-35-carboxylate |
| GRAZ-024 | 1206524-77-7 | (1R,2R)-2-(pent-4-en-1-yl)cyclopropan-1-ol |
| GRAZ-043 | 1703754-98-6 | 1-((1R,2R)-2-(pent-4-en-1-yl)cyclopropyl)ethan-1-one |
| GRAZ-044 | 1425038-20-5 | methyl (2S,4R)-4-((3-chloro-7-methoxyquinoxalin-2-yl)oxy)pyrrolidine-2-carboxylate methanesulfonate |
| GRAZ-045 | 1184-88-9 | sodium pivalate |
常见问题（FAQ）
Grazoprevir Hydrate的适应症有哪些？
已批准的适应症包括：丙型肝炎。
Grazoprevir Hydrate的专利什么时候到期？
Grazoprevir Hydrate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。
Grazoprevir Hydrate有几条合成路线？
本站收录 4 条合成路线，最短路线 4 步、总收率 60 mg。每条路线的中间体均带登记编号与 CAS 号。
Grazoprevir Hydrate的关键中间体在哪里可以采购？
Grazoprevir Hydrate的多条路线中间体已挂接 CAS 档案，其中 1 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Grazoprevir Hydrate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） · 2026-09-24