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比克恩丙诺
Tier B · 提前布局Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate
Gilead Inc
原研
2018
首批上市
-
到期年（公开口径）
$14.33B ▲
峰值销售
化学药
类型
靶点：HIV-1 RT、HIV integrase、RT
商品名：Biktarvy、必妥维
适应症（已批准）：HIV感染
各地区研发/上市状态
美国
批准上市
2018-02-07
欧盟
批准上市
2018-06-21
中国
批准上市
2019-08-02
日本
批准上市
2019-03-26
合成路线与中间体5 routes
原研路线 × 1优化路线（非专利）× 4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 7 · 总收率 33 mg
EMTR-0016117-80-2EMTR-002144967-77-1EMTR-003136831-95-3EMTR-00468-11-1EMTR-005136891-16-2EMTR-006—EMTR-007111878-21-8EMTR-008—EMTR-009143491-56-9API · 比克恩丙诺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EMTR-001 | 6117-80-2 | (Z)-but-2-ene-1,4-diol |
| EMTR-002 | 144967-77-1 | (Z)-but-2-ene-1,4-diyl dibutyrate |
| EMTR-003 | 136831-95-3 | 2-oxoethyl butyrate |
| EMTR-004 | 68-11-1 | 2-mercaptoacetic acid |
| EMTR-005 | 136891-16-2 | (5-oxo-1,3-oxathiolan-2-yl)methyl butyrate |
| EMTR-006 | - | (5-acetoxy-1,3-oxathiolan-2-yl)methyl butyrate |
| EMTR-007 | 111878-21-8 | 5-fluoro-N-(trimethylsilyl)-2-((trimethylsilyl)oxy)pyrimidin-4-amine |
| EMTR-008 | - | (5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl butyrate |
| EMTR-009 | 143491-56-9 | ((2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl butyrate |
优化Route 2步骤 10 · 总收率 5.5 mg
EMTR-01039281-67-9EMTR-011—EMTR-012139757-70-3EMTR-013140-89-6EMTR-014—EMTR-015139689-03-5EMTR-016139757-71-4EMTR-017—EMTR-018324015-67-0EMTR-019—EMTR-020—EMTR-021—API · 比克恩丙诺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EMTR-010 | 39281-67-9 | (2S,3S,4S,5S,6S)-6-(hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol |
| EMTR-011 | - | (2R,3S,4S,5R,6S)-6-((tosyloxy)methyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate |
| EMTR-012 | 139757-70-3 | (2R,3S,4S,5R,6S)-2-bromo-6-((tosyloxy)methyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate |
| EMTR-013 | 140-89-6 | potassium O-ethyl carbonodithioate |
| EMTR-014 | - | (2S,3S,4S)-8-oxa-6-thiabicyclo[3.2.1]octane-2,3,4-triol |
| EMTR-015 | 139689-03-5 | ((2R,5R)-5-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)-1,3-oxathiolan-2-yl)methanol |
| EMTR-016 | 139757-71-4 | (R)-1-((2R,5R)-2-(((tert-butyldiphenylsilyl)oxy)methyl)-1,3-oxathiolan-5-yl)ethane-1,2-diol |
| EMTR-017 | - | (2R)-2-(((tert-butyldiphenylsilyl)oxy)methyl)-1,3-oxathiolane-5-carboxylic acid |
| EMTR-018 | 324015-67-0 | (2R)-2-(((tert-butyldiphenylsilyl)oxy)methyl)-1,3-oxathiolan-5-yl acetate |
| EMTR-019 | - | N-(5-fluoro-2-((trimethylsilyl)oxy)pyrimidin-4-yl)acetamide |
| EMTR-020 | - | N-(1-((2R,5S)-2-(((tert-butyldiphenylsilyl)oxy)methyl)-1,3-oxathiolan-5-yl)-5-fluoro-2-oxo-1,2-dihydropyrimidin-4-yl)acetamide |
| EMTR-021 | - | 4-amino-1-((2R,5S)-2-(((tert-butyldiphenylsilyl)oxy)methyl)-1,3-oxathiolan-5-yl)-5-fluoropyrimidin-2(1H)-one |
优化Route 3步骤 6 · 总收率 20 mg
EMTR-019—EMTR-02240018-26-6EMTR-02364904-47-8EMTR-024146726-76-3EMTR-025—EMTR-026144371-00-6EMTR-027—EMTR-028156198-94-6API · 比克恩丙诺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EMTR-019 | - | N-(5-fluoro-2-((trimethylsilyl)oxy)pyrimidin-4-yl)acetamide |
| EMTR-022 | 40018-26-6 | 1,4-dithiane-2,5-diol |
| EMTR-023 | 64904-47-8 | 2-oxoethyl benzoate |
| EMTR-024 | 146726-76-3 | (5-acetoxy-1,3-oxathiolan-2-yl)methyl benzoate |
| EMTR-025 | - | (5-(4-acetamido-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl benzoate |
| EMTR-026 | 144371-00-6 | 4-amino-5-fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one |
| EMTR-027 | - | (5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl dihydrogen phosphate |
| EMTR-028 | 156198-94-6 | ((2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl dihydrogen phosphate |
优化Route 4步骤 5 · 总收率 45 mg
EMTR-02240018-26-6EMTR-029298-12-4EMTR-030672952-08-8EMTR-031147027-43-8EMTR-03289-78-1EMTR-033147027-09-6EMTR-0342022-85-7EMTR-035764659-72-5API · 比克恩丙诺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EMTR-022 | 40018-26-6 | 1,4-dithiane-2,5-diol |
| EMTR-029 | 298-12-4在售 | 2-oxoacetic acid |
| EMTR-030 | 672952-08-8 | 5-hydroxy-1,3-oxathiolane-2-carboxylic acid |
| EMTR-031 | 147027-43-8 | (2R,5R)-5-acetoxy-1,3-oxathiolane-2-carboxylic acid |
| EMTR-032 | 89-78-1在售 | (1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol |
| EMTR-033 | 147027-09-6 | (2R,5R)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-acetoxy-1,3-oxathiolane-2-carboxylate |
| EMTR-034 | 2022-85-7 | 4-amino-5-fluoropyrimidin-2(1H)-one |
| EMTR-035 | 764659-72-5 | (1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate |
优化Route 5步骤 6 · 总收率 80 g
EMTR-007111878-21-8EMTR-02240018-26-6EMTR-029298-12-4EMTR-03289-78-1EMTR-03626315-61-7EMTR-037—EMTR-0381020151-61-4EMTR-039764659-73-6EMTR-040258832-61-0API · 比克恩丙诺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EMTR-007 | 111878-21-8 | 5-fluoro-N-(trimethylsilyl)-2-((trimethylsilyl)oxy)pyrimidin-4-amine |
| EMTR-022 | 40018-26-6 | 1,4-dithiane-2,5-diol |
| EMTR-029 | 298-12-4在售 | 2-oxoacetic acid |
| EMTR-032 | 89-78-1在售 | (1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol |
| EMTR-036 | 26315-61-7 | (1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 2-oxoacetate |
| EMTR-037 | - | (2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate |
| EMTR-038 | 1020151-61-4 | (1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5R)-5-chloro-1,3-oxathiolane-2-carboxylate |
| EMTR-039 | 764659-73-6 | (1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate oxalate |
| EMTR-040 | 258832-61-0 | 4-amino-5-fluoro-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one hydrochloride |
常见问题（FAQ）
比克恩丙诺的适应症有哪些？
已批准的适应症包括：HIV感染。
比克恩丙诺的专利什么时候到期？
比克恩丙诺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。
比克恩丙诺有几条合成路线？
本站收录 5 条合成路线，最短路线 5 步、总收率 45 mg。每条路线的中间体均带登记编号与 CAS 号。
比克恩丙诺的关键中间体在哪里可以采购？
比克恩丙诺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。
如何获取比克恩丙诺中间体的报价？
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） · 2026-10-22