dolutegravir
Tivicay / Dovato · GSK / ViiV · HIV 整合酶
第二梯队 · 仅限已有工艺门槛 3/5
- US LOE
- 2028-02
- 备注
- 2028-02 档
- 准备期
- 2 年
- 年销售
- ~$1.9B+
- 关键中间体
- 1 个
门槛构成
HIV 整合酶 INSTI 平台与 Biktarvy INSTI 部分重叠
关键中间体链
本目录已覆盖 0/1INSTI 吡啶酮核心（与 Biktarvy 重叠）1335210-23-5 ✓ 路线核验路线节点 DOLU-022
依据：多替拉韦路线 DOLU-022 与比克替拉韦 BICTE-001 为同一 CAS 1335210-23-5 —— 客观印证了本库「平台化共享吡啶酮核心」的判断
未在目录中匹配 → 潜在新增供应机会
合成路线 · 中间体全表仅结构化数据（编号 / CAS / 分子式），路线由本站自行渲染
4 条路线 · 41 个节点 · 去重 CAS 33 个多替拉韦钠Dolutegravir Sodium原研 葛兰素史克drugId 22088316801683696454
原研路线 · 17 步 · 文献 US8129385B2 / WO2006116764A1优化路线 · 4 步 · 文献 WO2014128545A2 / EP2602260A1优化路线 · 12 步 · 文献 WO2010068262A1 / WO2010011819A1优化路线 · 7 步 · 总收率 2.67 g · 文献 J. Med. Chem. 2013, 56, 5901-5916 / EP2602260A1
| 编号 | CAS 号 | 分子式 | 分子量 | 英文名 / 结构描述 |
|---|---|---|---|---|
| DOLU-001 | 118-71-8 | C6H6O3 | 126.11 | 3-hydroxy-2-methyl-4H-pyran-4-one |
| DOLU-002 | 61049-69-2 | C13H12O3 | 216.23 | 3-(benzyloxy)-2-methyl-4H-pyran-4-one |
| DOLU-003 | 61160-18-7 | C13H13NO2 | 215.25 | 3-(benzyloxy)-2-methylpyridin-4(1H)-one |
| DOLU-004 | 906657-86-1 | C13H12BrNO2 | 294.14 | 3-(benzyloxy)-5-bromo-2-methylpyridin-4-ol |
| DOLU-005 | 906657-87-2 | C15H15NO4 | 273.28 | methyl 5-(benzyloxy)-4-hydroxy-6-methylnicotinate |
| DOLU-006 | 906657-88-3 | C17H17NO5 | 315.32 | methyl 4-acetoxy-5-(benzyloxy)-6-methylnicotinate |
| DOLU-007 | 906657-89-4 | C17H17NO6 | 331.32 | 4-acetoxy-3-(benzyloxy)-5-(methoxycarbonyl)-2-methylpyridine 1-oxide |
| DOLU-008 | 906657-90-7 | C19H19NO7 | 373.36 | methyl 4-acetoxy-6-(acetoxymethyl)-5-(benzyloxy)nicotinate |
| DOLU-009 | 未登记 | C16H15NO6 | 317.30 | 6-(acetoxymethyl)-5-(benzyloxy)-4-oxo-1,4-dihydropyridine-3-carboxylic acid |
| DOLU-010 | 72235-52-0 | C7H7F2N | 143.14 | (2,4-difluorophenyl)methanamine |
| DOLU-011 | 未登记 | C23H20F2N2O5 | 442.41 | 5-(benzyloxy)-N-(2,4-difluorobenzyl)-6-(hydroxymethyl)-4-oxo-1,4-dihydropyridine-3-carboxamide |
| DOLU-012 | 未登记 | C21H18F2N204 | 400.38 | 5-(benzyloxy)-N-(2,4-difluorobenzyl)-6-formyl-4-oxo-1,4-dihydropyridine-3-carboxamide |
| DOLU-013 | 未登记 | C21H16F2N2O4 | 398.36 | 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1,4-dihydropyridine-2-carboxylic acid |
| DOLU-014 | 未登记 | C21H16F2N2O5 | 414.36 | methyl 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-015 | 未登记 | C22H18F2N2O5 | 428.39 | methyl 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-016 | 106-95-6 | C3H5Br | 120.98 | 3-bromoprop-1-ene |
| DOLU-017 | 未登记 | C25H22F2N2O5 | 468.45 | methyl 1-allyl-3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-018 | 1229006-25-0 | C24H20F2N2O6 | 470.42 | methyl 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyridine-2-carboxylate |
| DOLU-019 | 61477-40-5 | C4H11NO | 89.14 | (R)-3-aminobutan-1-ol |
| DOLU-020 | 1206102-11-5 | C27H25F2N3O5 | 509.50 | (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-021 | 1646862-02-3 | C14H19NO8 | 329.30 | dimethyl 1-(2,2-dimethoxyethyl)-3-methoxy-4-oxo-1,4-dihydropyridine-2,5-dicarboxylate |
| DOLU-022 | 1335210-23-5 | C13H17NO8 | 315.28 | 1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid |
| DOLU-023 | 1623085-79-9 | C4H11NO·C4H6O6 | 239.22 | (R)-3-aminobutan-1-ol (2S,3S)-2,3-dihydroxysuccinate |
| DOLU-024 | 1335210-34-8 | C14H16N2O6 | 308.29 | (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 | C21H21F2N3O5 | 433.41 | (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 |
| DOLU-026 | 1206102-04-6 | C20H18O4 | 322.35 | 3-(benzyloxy)-2-(2-hydroxy-2-phenylethyl)-4H-pyran-4-one |
| DOLU-027 | 1206102-05-7 | C20H16O3 | 304.34 | (E)-3-(benzyloxy)-2-styryl-4H-pyran-4-one |
| DOLU-028 | 119736-16-2 | C13H10O5 | 246.22 | 3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid |
| DOLU-029 | 616-30-8 | C3H9NO2 | 91.11 | 3-aminopropane-1,2-diol |
| DOLU-030 | 1206102-06-8 | C16H17NO6 | 319.31 | 3-(benzyloxy)-1-(2,3-dihydroxypropyl)-4-oxo-1,4-dihydropyridine-2-carboxylic acid |
| DOLU-031 | 1206102-07-9 | C17H19NO6 | 333.34 | methyl 3-(benzyloxy)-1-(2,3-dihydroxypropyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-032 | 1206102-08-0 | C16H17NO6 | 319.31 | methyl 3-(benzyloxy)-1-(2,2-dihydroxyethyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
| DOLU-033 | 1206102-09-1 | C19H20N2O4 | 340.37 | (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 | C19H19BrN2O4 | 419.27 | (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 |
| DOLU-035 | 32807-28-6 | C5H7ClO3 | 150.56 | methyl 4-chloro-3-oxobutanoate |
| DOLU-036 | 82961-76-0 | C12H14O4 | 222.24 | methyl 4-(benzyloxy)-3-oxobutanoate |
| DOLU-037 | 1246616-65-8 | C15H19NO4 | 277.32 | (Z)-methyl 4-(benzyloxy)-2-((dimethylamino)methylene)-3-oxobutanoate |
| DOLU-038 | 未登记 | C16H14O7 | 318.28 | dimethyl 3-(benzyloxy)-4-oxo-4H-pyran-2,5-dicarboxylate |
| DOLU-039 | 22483-09-6 | C4H11NO2 | 105.14 | 2,2-dimethoxyethanamine |
| DOLU-040 | 1357289-08-7 | C20H23NO8 | 405.40 | dimethyl 3-(benzyloxy)-1-(2,2-dimethoxyethyl)-4-oxo-1,4-dihydropyridine-2,5-dicarboxylate |
| DOLU-041 | 1229006-21-6 | C26H26F2N2O7 | 516.49 | methyl 3-(benzyloxy)-5-((2,4-difluorobenzyl)carbamoyl)-1-(2,2-dimethoxyethyl)-4-oxo-1,4-dihydropyridine-2-carboxylate |
数据来源：多源数据交叉核实，仅取结构化字段；本方未使用任何第三方路线图—— 本表由本站依据结构化数据自行渲染。 标注「未登记」者，为源数据该节点 CAS 字段为空，非本站遗漏。
下一步
① 剩余「待核实」片段人工复核（源数据未给名称者已列出来源，不做猜测） → ② 评估 DMF/CEP 注册路径（准备期 2 年）→ ③ 借 GEO/SEO 获客 + 领英外联仿制药 / CDMO 客户。
按选品与立项 SOP 复核初筛层：只用本库已有字段，客户关与商业关需人工录入
用评分器补全五关 ↗市场关 · 窗口不进
准备期 2 年 · 不足 3 年
US LOE 2028-02
市场关 · 峰值销售看情况
≈$1.9B · 看壁垒与用量（$1–3B）
公开口径 ~$1.9B+
供给关 · 稀缺程度看情况
位置尚在 · 梯队 T2（须已有工艺才做）
梯队判定：第二梯队 · 仅限已有工艺
技术关 · 门槛看情况
门槛 3/5 · 临界（需代差确认）
HIV 整合酶 INSTI 平台 · 与 Biktarvy INSTI 部分重叠
客户关待录入
海外客户触达与推进阶段未入库
需 ≥1 家原研/Biotech/欧美 CDMO，且 ≥2 家进入样品测试、审计或商务谈判
商业关待录入
单吨产值、账期与产能占用未入库
按单位产能毛利排序，不按单吨价格排序；账期与库存不成立即不做
市场关与供给关、技术关的结论由本库字段机械映射得出（映射口径见SOP 第 1 节）； 客户关与商业关不在本库数据范围内，须由商务与财务按 SOP 第 2 节逐条录入后才能出立项结论。
提示：LOE 日期与门槛为公开源交叉核实结果（2026-09-13），最终以原研专利登记与 FDA / EMA 官方公告为准。 关键中间体 CAS 与合成路线来自多源数据交叉核实，仅取结构化数据、逐条做存在性校验 （见
scripts/build-loe-routes.mjs）；标「待核实」者为尚未匹配或代码层未提供名称， 入库采纳前请再经一次人工复核。