Unibest 优贝德
登录 / 注册
← 返回专利悬崖列表

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
合成路线与中间体 Route 1
编号CAS 号中间体名称
POSA-007141113-41-9(R)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propane-1,2-diol
POSA-008170985-69-0(R)-2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl methanesulfonate
POSA-009150024-48-9(R)-1-((2-(2,4-difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole
POSA-010105-53-3在售diethyl malonate
POSA-011185961-40-4ethyl (5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)-2-oxotetrahydrofuran-3-carboxylate
POSA-012149809-38-1(R)-4-(2,4-difluorophenyl)-2-(hydroxymethyl)-5-(1H-1,2,4-triazol-1-yl)pentane-1,4-diol
POSA-013149809-40-5(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-014149809-43-8((3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate
POSA-015112559-81-64-(4-(4-nitrophenyl)piperazin-1-yl)phenol
POSA-016161532-52-11-(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-017184378-04-94-(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-0181885-14-9在售phenyl carbonochloridate
POSA-019161532-54-3phenyl (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-020161532-55-4N-(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-021161532-56-54-(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-022170985-80-5(2S,3R)-2-((benzyloxy)methoxy)pentan-3-yl 4-bromobenzenesulfonate
POSA-00151336-94-82-chloro-1-(2,4-difluorophenyl)ethan-1-one
POSA-002122263-03-02-(2,4-difluorophenyl)-2-oxoethyl acetate
POSA-003149809-34-72-(2,4-difluorophenyl)allyl acetate
POSA-004141113-36-22-(2,4-difluorophenyl)prop-2-en-1-ol
POSA-005141113-37-3(S)-(2-(2,4-difluorophenyl)oxiran-2-yl)methanol
POSA-006288-88-0在售1H-1,2,4-triazole
优化Route 2步骤 11 · 总收率 300.5 g
合成路线与中间体 Route 2
编号CAS 号中间体名称
POSA-017184378-04-94-(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-0181885-14-9在售phenyl carbonochloridate
POSA-019161532-54-3phenyl (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-023687-47-8ethyl (S)-2-hydroxypropanoate
POSA-024123-75-1pyrrolidine
POSA-025122151-38-6(S)-2-hydroxy-1-(pyrrolidin-1-yl)propan-1-one
POSA-026122151-32-0(S)-2-(benzyloxy)-1-(pyrrolidin-1-yl)propan-1-one
POSA-027132489-33-9(S)-2-(benzyloxy)pentan-3-one
POSA-0281822329-44-1(2S)-2-(benzyloxy)pentan-3-ol
POSA-02998-57-71-chloro-4-(methylsulfonyl)benzene
POSA-030183871-33-2(2S)-2-(benzyloxy)pentan-3-yl 4-chlorobenzenesulfonate
POSA-0311250377-81-1((2S,3S)-2-(benzyloxy)pentan-3-yl)hydrazine (2R,3R)-2,3-bis(benzoyloxy)succinate
POSA-032170985-85-0N'-((2S,3S)-2-(benzyloxy)pentan-3-yl)formohydrazide
POSA-033170985-86-14-(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-03574853-08-04-(4-(4-aminophenyl)piperazin-1-yl)phenol
优化Route 3步骤 4 · 总收率 /
合成路线与中间体 Route 3
编号CAS 号中间体名称
POSA-014149809-43-8((3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate
POSA-033170985-86-14-(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-036454479-38-02-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-bromophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
POSA-037110-85-0在售piperazine
POSA-038454479-39-12-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-(piperazin-1-yl)phenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
POSA-039454479-36-81-(((2R,4R)-4-((4-bromophenoxy)methyl)-2-(2,4-difluorophenyl)tetrahydrofuran-2-yl)methyl)-1H-1,2,4-triazole
POSA-040106-41-24-bromophenol
优化Route 4步骤 7 · 总收率 300.5 g
合成路线与中间体 Route 4
编号CAS 号中间体名称
POSA-014149809-43-8((3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate
POSA-015112559-81-64-(4-(4-nitrophenyl)piperazin-1-yl)phenol
POSA-017184378-04-94-(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-0181885-14-9在售phenyl carbonochloridate
POSA-019161532-54-3phenyl (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-032170985-85-0N'-((2S,3S)-2-(benzyloxy)pentan-3-yl)formohydrazide
POSA-033170985-86-14-(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-03574853-08-04-(4-(4-aminophenyl)piperazin-1-yl)phenol
POSA-041104-94-94-methoxyaniline
POSA-04255743-71-0N,N-bis(2-chloroethyl)-4-nitroaniline
POSA-04374852-61-21-(4-methoxyphenyl)-4-(4-nitrophenyl)piperazine
优化Route 5步骤 10 · 总收率 /
合成路线与中间体 Route 5
编号CAS 号中间体名称
POSA-054170985-84-9(S,E)-N'-(2-(benzyloxy)propylidene)formohydrazide
POSA-014149809-43-8((3S,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate
POSA-0181885-14-9在售phenyl carbonochloridate
POSA-032170985-85-0N'-((2S,3S)-2-(benzyloxy)pentan-3-yl)formohydrazide
POSA-033170985-86-14-(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-036454479-38-02-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-bromophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
POSA-044184177-81-9phenyl (4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)carbamate
POSA-045184177-83-12-((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-046547-64-8methyl 2-hydroxypropanoate
POSA-047100-44-7(chloromethyl)benzene
POSA-04853346-03-5methyl 2-(benzyloxy)propanoate
POSA-0492627-86-3(S)-1-phenylethan-1-amine
POSA-0501428785-96-9(S)-1-phenylethan-1-amine (S)-2-(benzyloxy)propanoate
POSA-05177287-11-7methyl (S)-2-(benzyloxy)propanoate
POSA-05281445-44-5(S)-2-(benzyloxy)propanal
POSA-053624-84-0formohydrazide

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