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泊沙康唑
Tier C · 观察 / 贸易Posaconazole
Merck & Co Inc
原研
2005
首批上市
-
到期年(公开口径)
$0.74B ▲
峰值销售
化学药
类型
靶点:CYP51A1
商品名:Posanol、Spriafil、Noxafil、诺科飞、丰海畅、Posaconazole SP
适应症(已批准):念珠菌病、曲霉菌属感染、真菌感染、口腔念珠菌病、球孢菌病
各地区研发/上市状态
美国
批准上市
2006-09-15
欧盟
批准上市
2005-10-25
中国
批准上市
2013-06-03
日本
批准上市
2020-01-23
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 17 · 总收率 0.26 g

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| POSA-007 | 141113-41-9 | (R)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propane-1,2-diol |
| POSA-008 | 170985-69-0 | (R)-2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl methanesulfonate |
| POSA-009 | 150024-48-9 | (R)-1-((2-(2,4-difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole |
| POSA-010 | 105-53-3在售 | diethyl malonate |
| POSA-011 | 185961-40-4 | ethyl (5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)-2-oxotetrahydrofuran-3-carboxylate |
| POSA-012 | 149809-38-1 | (R)-4-(2,4-difluorophenyl)-2-(hydroxymethyl)-5-(1H-1,2,4-triazol-1-yl)pentane-1,4-diol |
| POSA-013 | 149809-40-5 | (R)-2-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)propane-1,3-diyl bis(4-methylbenzenesulfonate) |
| POSA-014 | 149809-43-8 | ((3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate |
| POSA-015 | 112559-81-6 | 4-(4-(4-nitrophenyl)piperazin-1-yl)phenol |
| POSA-016 | 161532-52-1 | 1-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)-4-(4-nitrophenyl)piperazine |
| POSA-017 | 184378-04-9 | 4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)aniline |
| POSA-018 | 1885-14-9在售 | phenyl carbonochloridate |
| POSA-019 | 161532-54-3 | phenyl (4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)carbamate |
| POSA-020 | 161532-55-4 | N-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)hydrazinecarboxamide |
| POSA-021 | 161532-56-5 | 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-022 | 170985-80-5 | (2S,3R)-2-((benzyloxy)methoxy)pentan-3-yl 4-bromobenzenesulfonate |
| POSA-001 | 51336-94-8 | 2-chloro-1-(2,4-difluorophenyl)ethan-1-one |
| POSA-002 | 122263-03-0 | 2-(2,4-difluorophenyl)-2-oxoethyl acetate |
| POSA-003 | 149809-34-7 | 2-(2,4-difluorophenyl)allyl acetate |
| POSA-004 | 141113-36-2 | 2-(2,4-difluorophenyl)prop-2-en-1-ol |
| POSA-005 | 141113-37-3 | (S)-(2-(2,4-difluorophenyl)oxiran-2-yl)methanol |
| POSA-006 | 288-88-0在售 | 1H-1,2,4-triazole |
优化Route 2步骤 11 · 总收率 300.5 g

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| POSA-017 | 184378-04-9 | 4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)aniline |
| POSA-018 | 1885-14-9在售 | phenyl carbonochloridate |
| POSA-019 | 161532-54-3 | phenyl (4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)carbamate |
| POSA-023 | 687-47-8 | ethyl (S)-2-hydroxypropanoate |
| POSA-024 | 123-75-1 | pyrrolidine |
| POSA-025 | 122151-38-6 | (S)-2-hydroxy-1-(pyrrolidin-1-yl)propan-1-one |
| POSA-026 | 122151-32-0 | (S)-2-(benzyloxy)-1-(pyrrolidin-1-yl)propan-1-one |
| POSA-027 | 132489-33-9 | (S)-2-(benzyloxy)pentan-3-one |
| POSA-028 | 1822329-44-1 | (2S)-2-(benzyloxy)pentan-3-ol |
| POSA-029 | 98-57-7 | 1-chloro-4-(methylsulfonyl)benzene |
| POSA-030 | 183871-33-2 | (2S)-2-(benzyloxy)pentan-3-yl 4-chlorobenzenesulfonate |
| POSA-031 | 1250377-81-1 | ((2S,3S)-2-(benzyloxy)pentan-3-yl)hydrazine (2R,3R)-2,3-bis(benzoyloxy)succinate |
| POSA-032 | 170985-85-0 | N'-((2S,3S)-2-(benzyloxy)pentan-3-yl)formohydrazide |
| POSA-033 | 170985-86-1 | 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-(benzyloxy)pentan-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-034 | - | - |
| POSA-035 | 74853-08-0 | 4-(4-(4-aminophenyl)piperazin-1-yl)phenol |
优化Route 3步骤 4 · 总收率 /

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| POSA-014 | 149809-43-8 | ((3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate |
| POSA-033 | 170985-86-1 | 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-(benzyloxy)pentan-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-036 | 454479-38-0 | 2-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-bromophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-037 | 110-85-0在售 | piperazine |
| POSA-038 | 454479-39-1 | 2-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-(piperazin-1-yl)phenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-039 | 454479-36-8 | 1-(((2R,4R)-4-((4-bromophenoxy)methyl)-2-(2,4-difluorophenyl)tetrahydrofuran-2-yl)methyl)-1H-1,2,4-triazole |
| POSA-040 | 106-41-2 | 4-bromophenol |
优化Route 4步骤 7 · 总收率 300.5 g

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| POSA-014 | 149809-43-8 | ((3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate |
| POSA-015 | 112559-81-6 | 4-(4-(4-nitrophenyl)piperazin-1-yl)phenol |
| POSA-017 | 184378-04-9 | 4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)aniline |
| POSA-018 | 1885-14-9在售 | phenyl carbonochloridate |
| POSA-019 | 161532-54-3 | phenyl (4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)carbamate |
| POSA-032 | 170985-85-0 | N'-((2S,3S)-2-(benzyloxy)pentan-3-yl)formohydrazide |
| POSA-033 | 170985-86-1 | 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-(benzyloxy)pentan-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-035 | 74853-08-0 | 4-(4-(4-aminophenyl)piperazin-1-yl)phenol |
| POSA-041 | 104-94-9 | 4-methoxyaniline |
| POSA-042 | 55743-71-0 | N,N-bis(2-chloroethyl)-4-nitroaniline |
| POSA-043 | 74852-61-2 | 1-(4-methoxyphenyl)-4-(4-nitrophenyl)piperazine |
优化Route 5步骤 10 · 总收率 /

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| POSA-054 | 170985-84-9 | (S,E)-N'-(2-(benzyloxy)propylidene)formohydrazide |
| POSA-014 | 149809-43-8 | ((3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate |
| POSA-018 | 1885-14-9在售 | phenyl carbonochloridate |
| POSA-032 | 170985-85-0 | N'-((2S,3S)-2-(benzyloxy)pentan-3-yl)formohydrazide |
| POSA-033 | 170985-86-1 | 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-(benzyloxy)pentan-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-036 | 454479-38-0 | 2-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-bromophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-044 | 184177-81-9 | phenyl (4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)carbamate |
| POSA-045 | 184177-83-1 | 2-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one |
| POSA-046 | 547-64-8 | methyl 2-hydroxypropanoate |
| POSA-047 | 100-44-7 | (chloromethyl)benzene |
| POSA-048 | 53346-03-5 | methyl 2-(benzyloxy)propanoate |
| POSA-049 | 2627-86-3 | (S)-1-phenylethan-1-amine |
| POSA-050 | 1428785-96-9 | (S)-1-phenylethan-1-amine (S)-2-(benzyloxy)propanoate |
| POSA-051 | 77287-11-7 | methyl (S)-2-(benzyloxy)propanoate |
| POSA-052 | 81445-44-5 | (S)-2-(benzyloxy)propanal |
| POSA-053 | 624-84-0 | formohydrazide |
常见问题(FAQ)
泊沙康唑的适应症有哪些?
已批准的适应症包括:念珠菌病、曲霉菌属感染、真菌感染、口腔念珠菌病、球孢菌病。
泊沙康唑的专利什么时候到期?
泊沙康唑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。
泊沙康唑有几条合成路线?
本站收录 5 条合成路线,最短路线 4 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
泊沙康唑的关键中间体在哪里可以采购?
泊沙康唑的多条路线中间体已挂接 CAS 档案,其中 4 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。
如何获取泊沙康唑中间体的报价?
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