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多替拉韦钠
Tier B — Position earlyDolutegravir Sodium
葛兰素史克
Originator
2013
First approval
-
Expiry (public)
$2.18B ▲
Peak sales
化学药
Type
Targets：HIV integrase
Brand：Tivicay PD、Tivicay、特威凯
Indications (approved)：HIV感染
Regional status
US
批准上市
2013-08-12
EU
批准上市
2014-01-16
China
批准上市
2015-12-30
Japan
批准上市
2014-03-24
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 17 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| DOLU-001 | 118-71-8 | 3-hydroxy-2-methyl-4H-pyran-4-one |
| DOLU-002 | 61049-69-2 | 3-(benzyloxy)-2-methyl-4H-pyran-4-one |
| DOLU-003 | 61160-18-7 | 3-(benzyloxy)-2-methylpyridin-4(1H)-one |
| DOLU-004 | 906657-86-1 | 3-(benzyloxy)-5-bromo-2-methylpyridin-4-ol |
| DOLU-005 | 906657-87-2 | methyl 5-(benzyloxy)-4-hydroxy-6-methylnicotinate |
| DOLU-006 | 906657-88-3 | methyl 4-acetoxy-5-(benzyloxy)-6-methylnicotinate |
| DOLU-007 | 906657-89-4 | 4-acetoxy-3-(benzyloxy)-5-(methoxycarbonyl)-2-methylpyridine 1-oxide |
| DOLU-008 | 906657-90-7 | methyl 4-acetoxy-6-(acetoxymethyl)-5-(benzyloxy)nicotinate |
| DOLU-009 | - | 6-(acetoxymethyl)-5-(benzyloxy)-4-oxo-1,4-dihydropyridine-3-carboxylic acid |
| DOLU-010 | 72235-52-0 | (2,4-difluorophenyl)methanamine |
| DOLU-011 | - | 5-(benzyloxy)-N-(2,4-difluorobenzyl)-6-(hydroxymethyl)-4-oxo-1,4-dihydropyridine-3-carboxamide |
| DOLU-012 | - | 5-(benzyloxy)-N-(2,4-difluorobenzyl)-6-formyl-4-oxo-1,4-dihydropyridine-3-carboxamide |
| DOLU-013 | - | 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1,4-dihydropyridine-2-carboxylic acid |
| DOLU-014 | - | methyl 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-015 | - | methyl 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-016 | 106-95-6Available | 3-bromoprop-1-ene |
| DOLU-017 | - | methyl 1-allyl-3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-018 | 1229006-25-0 | methyl 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyridine-2-carboxylate |
| DOLU-019 | 61477-40-5 | (R)-3-aminobutan-1-ol |
| DOLU-020 | 1206102-11-5 | (4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide |
OptimisedRoute 2Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| DOLU-010 | 72235-52-0 | (2,4-difluorophenyl)methanamine |
| DOLU-021 | 1646862-02-3 | dimethyl 1-(2,2-dimethoxyethyl)-3-methoxy-4-oxo-1,4-dihydropyridine-2,5-dicarboxylate |
| DOLU-022 | 1335210-23-5Available | 1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid |
| DOLU-023 | 1623085-79-9 | (R)-3-aminobutan-1-ol (2S,3S)-2,3-dihydroxysuccinate |
| DOLU-024 | 1335210-34-8 | (4R,12aS)-7-methoxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylic acid |
| DOLU-025 | 1335210-35-9 | (4R,12aS)-N-(2,4-difluorobenzyl)-7-methoxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide |
OptimisedRoute 3Steps 12 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| DOLU-001 | 118-71-8 | 3-hydroxy-2-methyl-4H-pyran-4-one |
| DOLU-002 | 61049-69-2 | 3-(benzyloxy)-2-methyl-4H-pyran-4-one |
| DOLU-010 | 72235-52-0 | (2,4-difluorophenyl)methanamine |
| DOLU-019 | 61477-40-5 | (R)-3-aminobutan-1-ol |
| DOLU-020 | 1206102-11-5 | (4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide |
| DOLU-026 | 1206102-04-6 | 3-(benzyloxy)-2-(2-hydroxy-2-phenylethyl)-4H-pyran-4-one |
| DOLU-027 | 1206102-05-7 | (E)-3-(benzyloxy)-2-styryl-4H-pyran-4-one |
| DOLU-028 | 119736-16-2 | 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid |
| DOLU-029 | 616-30-8 | 3-aminopropane-1,2-diol |
| DOLU-030 | 1206102-06-8 | 3-(benzyloxy)-1-(2,3-dihydroxypropyl)-4-oxo-1,4-dihydropyridine-2-carboxylic acid |
| DOLU-031 | 1206102-07-9 | methyl 3-(benzyloxy)-1-(2,3-dihydroxypropyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-032 | 1206102-08-0 | methyl 3-(benzyloxy)-1-(2,2-dihydroxyethyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-033 | 1206102-09-1 | (4R,12aS)-7-(benzyloxy)-4-methyl-3,4,12,12a-tetrahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-6,8-dione |
| DOLU-034 | 1206102-10-4 | (4R,12aS)-7-(benzyloxy)-9-bromo-4-methyl-3,4,12,12a-tetrahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-6,8-dione |
OptimisedRoute 4Steps 7 · Total yield 2.67 g
| Code | CAS No. | Intermediate |
|---|---|---|
| DOLU-010 | 72235-52-0 | (2,4-difluorophenyl)methanamine |
| DOLU-019 | 61477-40-5 | (R)-3-aminobutan-1-ol |
| DOLU-020 | 1206102-11-5 | (4R,12aS)-7-(benzyloxy)-N-(2,4-difluorobenzyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide |
| DOLU-035 | 32807-28-6 | methyl 4-chloro-3-oxobutanoate |
| DOLU-036 | 82961-76-0 | methyl 4-(benzyloxy)-3-oxobutanoate |
| DOLU-037 | 1246616-65-8 | (Z)-methyl 4-(benzyloxy)-2-((dimethylamino)methylene)-3-oxobutanoate |
| DOLU-038 | - | dimethyl 3-(benzyloxy)-4-oxo-4H-pyran-2,5-dicarboxylate |
| DOLU-039 | 22483-09-6 | 2,2-dimethoxyethanamine |
| DOLU-040 | 1357289-08-7 | dimethyl 3-(benzyloxy)-1-(2,2-dimethoxyethyl)-4-oxo-1,4-dihydropyridine-2,5-dicarboxylate |
| DOLU-041 | 1229006-21-6 | methyl 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-1-(2,2-dimethoxyethyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
Frequently asked questions
What are the approved indications of Dolutegravir Sodium?
Approved indications include: HIV感染.
When does the Dolutegravir Sodium patent expire?
No public expiry year is available for Dolutegravir Sodium yet; this page updates once verified.
How many synthesis routes are recorded for Dolutegravir Sodium?
4 synthesis routes are recorded; the shortest is 4 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Dolutegravir Sodium intermediates?
2 intermediate CAS of Dolutegravir Sodium 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 Dolutegravir Sodium 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