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Grazoprevir Hydrate
Tier C — Watch / tradeGrazoprevir Hydrate
默沙东
Originator
2016
First approval
-
Expiry (public)
No sales data
Peak sales
化学药
Type
Targets：NS3/NS4A
Brand：Grazyna
Indications (approved)：丙型肝炎
Regional status
US
-
EU
无进展
2016-06-01
China
临床一期
2013-11-19
Japan
批准上市
2016-09-28
Synthetic routes & intermediates4 routes
Originator routes × 1Optimised (non-patent) × 3Process 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 18 · Total yield 393 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 13682-77-4Available | 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 |
OptimisedRoute 2Steps 6 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 3Steps 10 · Total yield 694 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | - |
OptimisedRoute 4Steps 4 · Total yield 60 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
Frequently asked questions
What are the approved indications of Grazoprevir Hydrate?
Approved indications include: 丙型肝炎.
When does the Grazoprevir Hydrate patent expire?
No public expiry year is available for Grazoprevir Hydrate yet; this page updates once verified.
How many synthesis routes are recorded for Grazoprevir Hydrate?
4 synthesis routes are recorded; the shortest is 4 steps with 60 mg total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Grazoprevir Hydrate intermediates?
1 intermediate CAS of Grazoprevir Hydrate 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 Grazoprevir Hydrate 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) · 2026-09-24