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特拉匹韦
Tier B — Position earlyTelaprevir
Vertex Pharmaceuticals Incorporated
Originator
2011
First approval
-
Expiry (public)
$1.67B ▲
Peak sales
化学药
Type
Targets：NS3/NS4A
Brand：Incivek、Incivo、Telavic
Indications (approved)：丙型肝炎
Regional status
US
撤市
EU
无进展
2008-03-01
China
终止
2012-06-19
Japan
批准上市
2011-09-26
Synthetic routes & intermediates5 routes
Originator routes × 1Optimised (non-patent) × 4Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OriginatorRoute 1Steps 6 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 2Steps 8 · Total yield 16.6 g
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 3Steps 9 · Total yield 61.1 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 86483-52-5Available | 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 |
OptimisedRoute 4Steps 10 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 5Steps 12 · Total yield 6.28 g
| Code | CAS No. | Intermediate |
|---|---|---|
| TELAP-002 | 98-97-5 | pyrazine-2-carboxylic acid |
| TELAP-021 | 86483-52-5Available | cyclopropanamine |
| TELAP-040 | 627-05-4 | 1-nitrobutane |
| TELAP-041 | 298-12-4Available | 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 |
Frequently asked questions
What are the approved indications of Telaprevir?
Approved indications include: 丙型肝炎.
When does the Telaprevir patent expire?
No public expiry year is available for Telaprevir yet; this page updates once verified.
How many synthesis routes are recorded for Telaprevir?
5 synthesis routes are recorded; the shortest is 6 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Telaprevir intermediates?
2 intermediate CAS of Telaprevir are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.
How do I get a quote for Telaprevir intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-09-25