Invention Grant
- Patent Title: Simplified procedure for the preparation of darunavir
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Application No.: US16461754Application Date: 2017-11-16
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Publication No.: US10774088B2Publication Date: 2020-09-15
- Inventor: Alfred Elisabeth Stappers , Yolande Lydia Lang , Shane Barry Robinson
- Applicant: Janssen Sciences Ireland Unlimited Company
- Applicant Address: IE Co Cork
- Assignee: Janssen Sciences Ireland Unlimited Company
- Current Assignee: Janssen Sciences Ireland Unlimited Company
- Current Assignee Address: IE Co Cork
- Priority: com.zzzhc.datahub.patent.etl.us.BibliographicData$PriorityClaim@6e35d703
- International Application: PCT/EP2017/079375 WO 20171116
- International Announcement: WO2018/091559 WO 20180524
- Main IPC: C07D493/04
- IPC: C07D493/04

Abstract:
The present invention relates to an improved process for preparing [(1S,2R)-3-[[(4-aminophenyl)-sulfonyl](2-methyl-propyl)amino]-2-hydroxy-1-(phenylmethyl)-propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester—which compound is also known under its INN as darunavir—by reacting carbonic acid 2,5-dioxo-1-pyrrolidinyl[(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl]ester with 4-amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(2-methylpropyl)-benzenesulfonamide in ethanol as solvent. Furthermore said process allows for darunavir to be isolated immediately in its ethanolate form, i.e. darunavir monoethanolate, which is the marketed form of darunavir under the tradename Prezista™.
Public/Granted literature
- US20190359625A1 A SIMPLIFIED PROCEDURE FOR THE PREPARATION OF DARUNAVIR Public/Granted day:2019-11-28
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