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Anacetrapib
Tier C · 观察 / 贸易Anacetrapib
默沙东
原研
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首批上市
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到期年（公开口径）
无销量数据
峰值销售
化学药
类型
靶点：HDL-cholesterol、CETP
适应症（已批准）：高胆固醇血症、心脏和血管疾病、血脂障碍、动脉粥样硬化、II型高脂蛋白血症、纯合子家族性高胆固醇血症、高脂血症、冠状动脉疾病
各地区研发/上市状态
美国
临床三期
2015-07-14
欧盟
临床三期
2011-06-01
中国
临床三期
2014-10-22
日本
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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 15 · 总收率 3.50 g
ANAC-001163444-17-5ANAC-0026526-08-5ANAC-003868166-20-5ANAC-004702641-04-1ANAC-005702641-05-2ANAC-006702641-06-3ANAC-007875444-08-9ANAC-008875446-35-8ANAC-009875446-29-0ANAC-010401-95-6ANAC-01179-24-3ANAC-0121152029-00-9ANAC-013875444-02-3ANAC-014—ANAC-01574457-86-6ANAC-01696826-25-4ANAC-0171262414-96-9ANAC-018944317-92-4API · Anacetrapib
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANAC-001 | 163444-17-5 | 2-iodo-4-(trifluoromethyl)aniline |
| ANAC-002 | 6526-08-5 | 2-amino-5-(trifluoromethyl)benzonitrile |
| ANAC-003 | 868166-20-5 | 2-iodo-5-(trifluoromethyl)benzonitrile |
| ANAC-004 | 702641-04-1 | 2-iodo-5-(trifluoromethyl)benzoic acid |
| ANAC-005 | 702641-05-2 | [2-iodo-5-(trifluoromethyl)phenyl]methanol |
| ANAC-006 | 702641-06-3 | 2-(bromomethyl)-1-iodo-4-(trifluoromethyl)benzene |
| ANAC-007 | 875444-08-9 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one |
| ANAC-008 | 875446-35-8 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-3-(2-iodo-5-(trifluoromethyl)benzyl)-4-methyloxazolidin-2-one |
| ANAC-009 | 875446-29-0 | (4-fluoro-5-isopropyl-2-methoxyphenyl)boronic acid |
| ANAC-010 | 401-95-6 | 3,5-bis(trifluoromethyl)benzaldehyde |
| ANAC-011 | 79-24-3 | nitroethane |
| ANAC-012 | 1152029-00-9 | 1-(3,5-bis(trifluoromethyl)phenyl)-2-nitropropan-1-ol |
| ANAC-013 | 875444-02-3 | 2-amino-1-(3,5-bis(trifluoromethyl)phenyl)propan-1-ol |
| ANAC-014 | - | 5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one |
| ANAC-015 | 74457-86-6 | 1-(2-fluoro-4-methoxyphenyl)ethan-1-one |
| ANAC-016 | 96826-25-4 | 2-(2-fluoro-4-methoxyphenyl)propan-2-ol |
| ANAC-017 | 1262414-96-9 | 2-fluoro-1-isopropyl-4-methoxybenzene |
| ANAC-018 | 944317-92-4 | 1-bromo-4-fluoro-5-isopropyl-2-methoxybenzene |
优化Route 2步骤 11 · 总收率 4.40 kg
ANAC-001163444-17-5ANAC-0026526-08-5ANAC-003868166-20-5ANAC-004702641-04-1ANAC-005702641-05-2ANAC-007875444-08-9ANAC-009875446-29-0ANAC-019875548-97-3ANAC-020875551-28-3ANAC-0211142-20-7ANAC-0221117-97-1ANAC-023114744-83-1ANAC-024114744-83-1ANAC-025871917-79-2ANAC-026877384-16-2API · Anacetrapib
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANAC-001 | 163444-17-5 | 2-iodo-4-(trifluoromethyl)aniline |
| ANAC-002 | 6526-08-5 | 2-amino-5-(trifluoromethyl)benzonitrile |
| ANAC-003 | 868166-20-5 | 2-iodo-5-(trifluoromethyl)benzonitrile |
| ANAC-004 | 702641-04-1 | 2-iodo-5-(trifluoromethyl)benzoic acid |
| ANAC-005 | 702641-05-2 | [2-iodo-5-(trifluoromethyl)phenyl]methanol |
| ANAC-007 | 875444-08-9 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one |
| ANAC-009 | 875446-29-0 | (4-fluoro-5-isopropyl-2-methoxyphenyl)boronic acid |
| ANAC-019 | 875548-97-3 | (4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methanol |
| ANAC-020 | 875551-28-3 | 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)-1,1'-biphenyl |
| ANAC-021 | 1142-20-7 | (S)-2-(((benzyloxy)carbonyl)amino)propanoic acid |
| ANAC-022 | 1117-97-1在售 | N,O-dimethylhydroxylamine |
| ANAC-023 | 114744-83-1 | 1-bromo-3,5-bis(trifluoromethyl)benzene |
| ANAC-024 | 114744-83-1 | 1-bromo-3,5-bis(trifluoromethyl)benzene |
| ANAC-025 | 871917-79-2 | benzyl (S)-(1-(3,5-bis(trifluoromethyl)phenyl)-1-oxopropan-2-yl)carbamate |
| ANAC-026 | 877384-16-2 | benzyl ((1R,2S)-1-(3,5-bis(trifluoromethyl)phenyl)-1-hydroxypropan-2-yl)carbamate |
优化Route 3步骤 9 · 总收率 /
ANAC-018944317-92-4ANAC-019875548-97-3ANAC-020875551-28-3ANAC-027348-57-2ANAC-028450-88-4ANAC-02975-36-5ANAC-030914221-54-8ANAC-031958029-46-4ANAC-032851513-74-1ANAC-033958029-47-5ANAC-03479-22-1ANAC-035—API · Anacetrapib
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANAC-018 | 944317-92-4 | 1-bromo-4-fluoro-5-isopropyl-2-methoxybenzene |
| ANAC-019 | 875548-97-3 | (4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methanol |
| ANAC-020 | 875551-28-3 | 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)-1,1'-biphenyl |
| ANAC-027 | 348-57-2 | 1-bromo-2,4-difluorobenzene |
| ANAC-028 | 450-88-4 | 1-bromo-4-fluoro-2-methoxybenzene |
| ANAC-029 | 75-36-5 | acetyl chloride |
| ANAC-030 | 914221-54-8 | 1-(5-bromo-2-fluoro-4-methoxyphenyl)ethan-1-one |
| ANAC-031 | 958029-46-4 | 2-(5-bromo-2-fluoro-4-methoxyphenyl)propan-2-ol |
| ANAC-032 | 851513-74-1 | 2-(3-(trifluoromethyl)phenyl)-4,5-dihydrooxazole |
| ANAC-033 | 958029-47-5 | 2-(4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)-4,5-dihydrooxazole |
| ANAC-034 | 79-22-1 | methyl carbonochloridate |
| ANAC-035 | - | methyl (2-chloroethyl)(4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-carbonyl)carbamate |
优化Route 4步骤 9 · 总收率 4.50 g
ANAC-005702641-05-2ANAC-009875446-29-0ANAC-019875548-97-3ANAC-0211142-20-7ANAC-024114744-83-1ANAC-025871917-79-2ANAC-026877384-16-2ANAC-036875551-32-9ANAC-0371152029-16-7ANAC-0381620289-77-1ANAC-0391220703-07-0ANAC-040110-91-8ANAC-041376581-13-4API · Anacetrapib
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANAC-005 | 702641-05-2 | [2-iodo-5-(trifluoromethyl)phenyl]methanol |
| ANAC-009 | 875446-29-0 | (4-fluoro-5-isopropyl-2-methoxyphenyl)boronic acid |
| ANAC-019 | 875548-97-3 | (4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methanol |
| ANAC-021 | 1142-20-7 | (S)-2-(((benzyloxy)carbonyl)amino)propanoic acid |
| ANAC-024 | 114744-83-1 | 1-bromo-3,5-bis(trifluoromethyl)benzene |
| ANAC-025 | 871917-79-2 | benzyl (S)-(1-(3,5-bis(trifluoromethyl)phenyl)-1-oxopropan-2-yl)carbamate |
| ANAC-026 | 877384-16-2 | benzyl ((1R,2S)-1-(3,5-bis(trifluoromethyl)phenyl)-1-hydroxypropan-2-yl)carbamate |
| ANAC-036 | 875551-32-9 | 4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-carbaldehyde |
| ANAC-037 | 1152029-16-7 | (1R,2S)-2-amino-1-(3,5-bis(trifluoromethyl)phenyl)propan-1-ol |
| ANAC-038 | 1620289-77-1 | (1R,2S)-1-(3,5-bis(trifluoromethyl)phenyl)-2-(((E)-(4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methylene)amino)propan-1-ol |
| ANAC-039 | 1220703-07-0 | (1R,2S)-1-(3,5-bis(trifluoromethyl)phenyl)-2-(((4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methyl)amino)propan-1-ol |
| ANAC-040 | 110-91-8在售 | morpholine |
| ANAC-041 | 376581-13-4 | benzyl (S)-(1-morpholino-1-oxopropan-2-yl)carbamate |
优化Route 5步骤 4 · 总收率 85.00 mg
ANAC-007875444-08-9ANAC-01179-24-3ANAC-020875551-28-3ANAC-04217352-25-9ANAC-0431480542-41-3ANAC-0441498289-59-0API · Anacetrapib
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANAC-007 | 875444-08-9 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one |
| ANAC-011 | 79-24-3 | nitroethane |
| ANAC-020 | 875551-28-3 | 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)-1,1'-biphenyl |
| ANAC-042 | 17352-25-9 | 3,5-diiodobenzaldehyde |
| ANAC-043 | 1480542-41-3 | (1R,2S)-1-(3,5-diiodophenyl)-2-nitropropan-1-ol |
| ANAC-044 | 1498289-59-0 | (4S,5R)-5-(3,5-diiodophenyl)-4-methyloxazolidin-2-one |
常见问题（FAQ）
Anacetrapib的适应症有哪些？
已批准的适应症包括：高胆固醇血症、心脏和血管疾病、血脂障碍、动脉粥样硬化、II型高脂蛋白血症、纯合子家族性高胆固醇血症、高脂血症、冠状动脉疾病。
Anacetrapib的专利什么时候到期？
Anacetrapib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。
Anacetrapib有几条合成路线？
本站收录 5 条合成路线，最短路线 4 步、总收率 85.00 mg。每条路线的中间体均带登记编号与 CAS 号。
Anacetrapib的关键中间体在哪里可以采购？
Anacetrapib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Anacetrapib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