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多替拉韦钠
Tier B · 提前布局Dolutegravir Sodium
葛兰素史克
原研
2013
首批上市
-
到期年（公开口径）
$2.18B ▲
峰值销售
化学药
类型
靶点：HIV integrase
商品名：Tivicay PD、Tivicay、特威凯
适应症（已批准）：HIV感染
各地区研发/上市状态
美国
批准上市
2013-08-12
欧盟
批准上市
2014-01-16
中国
批准上市
2015-12-30
日本
批准上市
2014-03-24
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 17 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| 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 | 106-95-6在售 | 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 |
优化Route 2步骤 4 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| 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 | 1335210-23-5在售 | 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 |
优化Route 3步骤 12 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| 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 |
优化Route 4步骤 7 · 总收率 2.67 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| 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 |
常见问题（FAQ）
多替拉韦钠的适应症有哪些？
已批准的适应症包括：HIV感染。
多替拉韦钠的专利什么时候到期？
多替拉韦钠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。
多替拉韦钠有几条合成路线？
本站收录 4 条合成路线，最短路线 4 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
多替拉韦钠的关键中间体在哪里可以采购？
多替拉韦钠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。
如何获取多替拉韦钠中间体的报价？
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