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泊沙康唑
Tier C — Watch / tradePosaconazole
Merck & Co Inc
Originator
2005
First approval
-
Expiry (public)
$0.74B ▲
Peak sales
化学药
Type
Targets：CYP51A1
Brand：Posanol、Spriafil、Noxafil、诺科飞、丰海畅、Posaconazole SP
Indications (approved)：念珠菌病、曲霉菌属感染、真菌感染、口腔念珠菌病、球孢菌病
Regional status
US
批准上市
2006-09-15
EU
批准上市
2005-10-25
China
批准上市
2013-06-03
Japan
批准上市
2020-01-23
Synthetic routes & intermediates5 routes
Originator routes × 1Optimised (non-patent) × 4Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OriginatorRoute 1Steps 17 · Total yield 0.26 g
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 105-53-3Available | 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 | 1885-14-9Available | 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 | 288-88-0Available | 1H-1,2,4-triazole |
OptimisedRoute 2Steps 11 · Total yield 300.5 g
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 1885-14-9Available | 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 |
OptimisedRoute 3Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 110-85-0Available | 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 |
OptimisedRoute 4Steps 7 · Total yield 300.5 g
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 1885-14-9Available | 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 |
OptimisedRoute 5Steps 10 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 1885-14-9Available | 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 |
Frequently asked questions
What are the approved indications of Posaconazole?
Approved indications include: 念珠菌病, 曲霉菌属感染, 真菌感染, 口腔念珠菌病, 球孢菌病.
When does the Posaconazole patent expire?
No public expiry year is available for Posaconazole yet; this page updates once verified.
How many synthesis routes are recorded for Posaconazole?
5 synthesis routes are recorded; the shortest is 4 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Posaconazole intermediates?
4 intermediate CAS of Posaconazole are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.
How do I get a quote for Posaconazole intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-09-24