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特拉匹韦
Tier B · 提前布局Telaprevir
Vertex Pharmaceuticals Incorporated
原研
2011
首批上市
-
到期年（公开口径）
$1.67B ▲
峰值销售
化学药
类型
靶点：NS3/NS4A
商品名：Incivek、Incivo、Telavic
适应症（已批准）：丙型肝炎
各地区研发/上市状态
美国
撤市
欧盟
无进展
2008-03-01
中国
终止
2012-06-19
日本
批准上市
2011-09-26
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 6 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TELAP-001 | 402960-22-9 | methyl (S)-2-((S)-2-amino-2-cyclohexylacetamido)-3,3-dimethylbutanoate |
| TELAP-002 | 98-97-5 | pyrazine-2-carboxylic acid |
| TELAP-003 | 402958-95-6 | methyl (S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoate |
| TELAP-004 | 402958-96-7 | (S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoic acid |
| TELAP-005 | 402958-25-2 | ethyl (1S,3aR,6aS)-octahydrocyclopenta[c]pyrrole-1-carboxylate |
| TELAP-006 | 402958-97-8 | ethyl (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylate |
| TELAP-007 | 402958-98-9 | (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylic acid |
| TELAP-008 | 402960-19-4 | (3S)-3-amino-N-cyclopropyl-2-hydroxyhexanamide |
| TELAP-009 | 402959-36-8 | (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((3S)-1-(cyclopropylamino)-2-hydroxy-1-oxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide |
优化Route 2步骤 8 · 总收率 16.6 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TELAP-002 | 98-97-5 | pyrazine-2-carboxylic acid |
| TELAP-007 | 402958-98-9 | (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylic acid |
| TELAP-008 | 402960-19-4 | (3S)-3-amino-N-cyclopropyl-2-hydroxyhexanamide |
| TELAP-009 | 402959-36-8 | (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((3S)-1-(cyclopropylamino)-2-hydroxy-1-oxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide |
| TELAP-010 | 62965-10-0 | (S)-2-(((benzyloxy)carbonyl)amino)-3,3-dimethylbutanoic acid |
| TELAP-011 | 714194-68-0 | tert-butyl (1S,3aR,6aS)-octahydrocyclopenta[c]pyrrole-1-carboxylate |
| TELAP-012 | 926276-15-5 | tert-butyl (1S,3aR,6aS)-2-((S)-2-(((benzyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylate |
| TELAP-013 | 926276-16-6 | tert-butyl (1S,3aR,6aS)-2-((S)-2-amino-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylate |
| TELAP-014 | 69901-75-3 | (S)-2-(((benzyloxy)carbonyl)amino)-2-cyclohexylacetic acid |
| TELAP-015 | 926276-17-7 | tert-butyl (1S,3aR,6aS)-2-((S)-2-((S)-2-(((benzyloxy)carbonyl)amino)-2-cyclohexylacetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylate |
| TELAP-016 | 926276-18-8 | tert-butyl (1S,3aR,6aS)-2-((S)-2-((S)-2-amino-2-cyclohexylacetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylate |
| TELAP-017 | 926276-19-9 | tert-butyl (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylate |
优化Route 3步骤 9 · 总收率 61.1 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TELAP-004 | 402958-96-7 | (S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoic acid |
| TELAP-009 | 402959-36-8 | (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((3S)-1-(cyclopropylamino)-2-hydroxy-1-oxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide |
| TELAP-018 | 2305-21-7 | (E)-hex-2-en-1-ol |
| TELAP-019 | 111003-36-2 | ((2R,3S)-3-propyloxiran-2-yl)methanol |
| TELAP-020 | 253783-29-8 | (2S,3S)-3-propyloxirane-2-carboxylic acid |
| TELAP-021 | 86483-52-5在售 | cyclopropanamine |
| TELAP-022 | 1644180-14-2 | (2S,3S)-N-cyclopropyl-3-propyloxirane-2-carboxamide |
| TELAP-023 | 950483-68-8 | (2S,3S)-3-azido-N-cyclopropyl-2-hydroxyhexanamide |
| TELAP-024 | 944716-73-8 | (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyhexanamide hydrochloride |
| TELAP-025 | 1414976-36-5 | (1S,3aR,6aS)-2-benzyloctahydrocyclopenta[c]pyrrole-1-carboxylic acid |
| TELAP-026 | 1644180-15-3 | (1S,3aR,6aS)-2-benzyl-N-((3S)-1-(cyclopropylamino)-2-hydroxy-1-oxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide |
| TELAP-027 | 1208221-46-8 | (1S,3aR,6aS)-N-((3S)-1-(cyclopropylamino)-2-hydroxy-1-oxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide |
优化Route 4步骤 10 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TELAP-002 | 98-97-5 | pyrazine-2-carboxylic acid |
| TELAP-003 | 402958-95-6 | methyl (S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoate |
| TELAP-004 | 402958-96-7 | (S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoic acid |
| TELAP-028 | 22724-81-8 | (S)-2-aminopentan-1-ol |
| TELAP-029 | 1257874-84-2 | (S)-N-(1-hydroxypentan-2-yl)formamide |
| TELAP-030 | 1257874-83-1 | (S)-N-(1-oxopentan-2-yl)formamide |
| TELAP-031 | 5500-21-0 | isocyanocyclopropane |
| TELAP-032 | 1257874-85-3 | (3S)-1-(cyclopropylamino)-3-formamido-1-oxohexan-2-yl acetate |
| TELAP-033 | - | (3S)-1-(cyclopropylamino)-3-isocyano-1-oxohexan-2-yl acetate |
| TELAP-034 | 1205676-33-0 | (3aS,6aR)-1,3a,4,5,6,6a-hexahydrocyclopenta[c]pyrrole |
| TELAP-035 | 1257874-86-4 | (3S)-3-((1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxamido)-1-(cyclopropylamino)-1-oxohexan-2-yl acetate |
| TELAP-036 | 145618-11-7 | methyl (S)-2-amino-2-cyclohexylacetate |
| TELAP-037 | 848777-29-7 | methyl (S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetate |
| TELAP-038 | 848777-30-0 | (S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetic acid |
| TELAP-039 | 63038-26-6 | methyl (S)-2-amino-3,3-dimethylbutanoate |
优化Route 5步骤 12 · 总收率 6.28 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| TELAP-002 | 98-97-5 | pyrazine-2-carboxylic acid |
| TELAP-021 | 86483-52-5在售 | cyclopropanamine |
| TELAP-040 | 627-05-4 | 1-nitrobutane |
| TELAP-041 | 298-12-4在售 | 2-oxoacetic acid |
| TELAP-042 | 1418311-53-1 | (3S)-2-hydroxy-3-nitrohexanoic acid |
| TELAP-043 | 402959-32-4 | (3S)-3-amino-2-hydroxyhexanoic acid |
| TELAP-044 | 1418311-54-2 | (3S)-3-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-2-hydroxyhexanoic acid |
| TELAP-045 | 1418311-52-0 | (S)-3-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-2-oxohexanoic acid |
| TELAP-046 | - | - |
| TELAP-047 | - | - |
| TELAP-048 | 1418311-56-4 | (1S,3aR,6aS)-2-(((9H-fluoren-9-yl)methoxy)carbonyl)octahydrocyclopenta[c]pyrrole-1-carboxylic acid |
| TELAP-049 | - | - |
| TELAP-050 | 132684-60-7 | (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-3,3-dimethylbutanoic acid |
| TELAP-051 | - | - |
| TELAP-052 | 161321-36-4 | (S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-2-cyclohexylacetic acid |
| TELAP-053 | - | - |
| TELAP-054 | - | - |
| TELAP-055 | 1418311-55-3 | (S)-3-((1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxamido)-2-oxohexanoic acid |
常见问题（FAQ）
特拉匹韦的适应症有哪些？
已批准的适应症包括：丙型肝炎。
特拉匹韦的专利什么时候到期？
特拉匹韦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。
特拉匹韦有几条合成路线？
本站收录 5 条合成路线，最短路线 6 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
特拉匹韦的关键中间体在哪里可以采购？
特拉匹韦的多条路线中间体已挂接 CAS 档案，其中 2 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。
如何获取特拉匹韦中间体的报价？
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