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考比司他
Tier C · 观察 / 贸易Cobicistat
Gilead Sciences Inc
原研
2013
首批上市
-
到期年（公开口径）
无销量数据
峰值销售
化学药
类型
靶点：CYP3A
商品名：Tybost
适应症（已批准）：HIV感染
各地区研发/上市状态
美国
撤市
欧盟
批准上市
2013-09-19
中国
-
日本
-
合成路线与中间体3 routes
原研路线 × 1优化路线（非专利）× 2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 10 · 总收率 580 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| COBI-001 | 154212-60-9 | 1-(2-isopropylthiazol-4-yl)-N-methylmethanamine |
| COBI-002 | 3350-15-0 | (S)-methyl 2-amino-4-((tert-butoxycarbonyl)amino)butanoate hydrochloride |
| COBI-003 | 1004316-83-9 | (S)-methyl 4-((tert-butoxycarbonyl)amino)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)butanoate |
| COBI-004 | 1004316-84-0 | (S)-4-((tert-butoxycarbonyl)amino)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)butanoic acid |
| COBI-005 | 1004316-18-0 | thiazol-5-ylmethyl ((2R,5R)-5-amino-1,6-diphenylhexan-2-yl)carbamate |
| COBI-006 | 1004316-85-1 | - |
| COBI-007 | 1004316-87-3 | thiazol-5-ylmethyl ((2R,5R)-5-((S)-4-amino-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)butanamido)-1,6-diphenylhexan-2-yl)carbamate |
| COBI-008 | 108385-55-3 | (S)-tert-butyl (1-phenyl-3-(phenylsulfonyl)propan-2-yl)carbamate |
| COBI-009 | 158380-76-8 | (S)-tert-butyl benzyl(1-oxo-3-phenylpropan-2-yl)carbamate |
| COBI-010 | 1004316-38-4 | tert-butyl benzyl((2S,5S)-5-((tert-butoxycarbonyl)amino)-3-hydroxy-1,6-diphenyl-4-(phenylsulfonyl)hexan-2-yl)carbamate |
| COBI-011 | 168846-63-7 | tert-butyl benzyl((2S,5S,E)-5-((tert-butoxycarbonyl)amino)-1,6-diphenylhex-3-en-2-yl)carbamate |
| COBI-012 | 168846-62-6 | di-tert-butyl ((2S,5S,E)-1,6-diphenylhex-3-ene-2,5-diyl)dicarbamate |
| COBI-013 | 144186-34-5 | (2R,5R)-1,6-diphenylhexane-2,5-diamine |
| COBI-014 | 144163-97-3 | 4-nitrophenyl (thiazol-5-ylmethyl) carbonate |
优化Route 2步骤 11 · 总收率 15.95 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| COBI-001 | 154212-60-9 | 1-(2-isopropylthiazol-4-yl)-N-methylmethanamine |
| COBI-005 | 1004316-18-0 | thiazol-5-ylmethyl ((2R,5R)-5-amino-1,6-diphenylhexan-2-yl)carbamate |
| COBI-013 | 144186-34-5 | (2R,5R)-1,6-diphenylhexane-2,5-diamine |
| COBI-014 | 144163-97-3 | 4-nitrophenyl (thiazol-5-ylmethyl) carbonate |
| COBI-015 | 6372-14-1 | (S)-benzyl (1-hydroxy-3-phenylpropan-2-yl)carbamate |
| COBI-016 | 137649-69-5 | dibenzyl ((2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl)dicarbamate |
| COBI-017 | 6160-65-2 | di(1H-imidazol-1-yl)methanethione |
| COBI-018 | 1004316-58-8 | dibenzyl ((1S,1'S)-((4R,5R)-2-thioxo-1,3-dioxolane-4,5-diyl)bis(2-phenylethane-1,1-diyl))dicarbamate |
| COBI-019 | 144163-56-4 | dibenzyl ((2S,5S,E)-1,6-diphenylhex-3-ene-2,5-diyl)dicarbamate |
| COBI-020 | 1004316-92-0 | (S)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanoic acid |
| COBI-021 | 1423796-11-5 | (S)-3-aminodihydrofuran-2(3H)-one hydrobromide |
| COBI-022 | 1004316-93-1 | (S)-1-((2-isopropylthiazol-4-yl)methyl)-1-methyl-3-(2-oxotetrahydrofuran-3-yl)urea |
| COBI-023 | - | (S)-benzyl 4-hydroxy-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)butanoate |
| COBI-024 | 1004316-95-3 | (S)-benzyl 2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-oxobutanoate |
| COBI-025 | 110-91-8在售 | morpholine |
| COBI-026 | 1004316-96-4 | (S)-benzyl 2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanoate |
优化Route 3步骤 12 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| COBI-001 | 154212-60-9 | 1-(2-isopropylthiazol-4-yl)-N-methylmethanamine |
| COBI-013 | 144186-34-5 | (2R,5R)-1,6-diphenylhexane-2,5-diamine |
| COBI-014 | 144163-97-3 | 4-nitrophenyl (thiazol-5-ylmethyl) carbonate |
| COBI-021 | 1423796-11-5 | (S)-3-aminodihydrofuran-2(3H)-one hydrobromide |
| COBI-022 | 1004316-93-1 | (S)-1-((2-isopropylthiazol-4-yl)methyl)-1-methyl-3-(2-oxotetrahydrofuran-3-yl)urea |
| COBI-025 | 110-91-8在售 | morpholine |
| COBI-027 | 73058-30-7 | (S)-2-benzylaziridine |
| COBI-028 | 13360-57-1 | dimethylsulfamoyl chloride |
| COBI-029 | 902146-43-4 | (S)-2-benzyl-N,N-dimethylaziridine-1-sulfonamide |
| COBI-030 | 1247119-27-2 | - |
| COBI-031 | 144163-57-5 | (2S,5S,E)-1,6-diphenylhex-3-ene-2,5-diamine |
| COBI-032 | 1247119-31-8 | (2R,5R)-1,6-diphenylhexane-2,5-diamine dihydrochloride |
| COBI-033 | 1247119-33-0 | thiazol-5-ylmethyl ((2R,5R)-5-amino-1,6-diphenylhexan-2-yl)carbamate hydrochloride |
| COBI-034 | 1169870-16-9 | potassium (S)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanoate |
| COBI-035 | 63-68-3 | (S)-2-amino-4-(methylthio)butanoic acid |
| COBI-036 | 1051461-77-8 | (S)-ethyl 4-iodo-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)butanoate |
| COBI-037 | 1247119-36-3 | (S)-ethyl 2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanoate oxalate |
常见问题（FAQ）
考比司他的适应症有哪些？
已批准的适应症包括：HIV感染。
考比司他的专利什么时候到期？
考比司他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。
考比司他有几条合成路线？
本站收录 3 条合成路线，最短路线 10 步、总收率 580 mg。每条路线的中间体均带登记编号与 CAS 号。
考比司他的关键中间体在哪里可以采购？
考比司他的多条路线中间体已挂接 CAS 档案，其中 1 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。
如何获取考比司他中间体的报价？
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