Invention Grant
- Patent Title: Methods for the preparation of drospirenone and intermediates thereof
- Patent Title (中): 屈螺酮的制备方法及其中间体
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Application No.: US13813195Application Date: 2011-07-22
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Publication No.: US08841283B2Publication Date: 2014-09-23
- Inventor: Mauro Montorsi , Edoardo Mariani , Luca Gambarin , Gianmauro Orru′ , Romeo Scalaprice , Massimo Merlo , Erika Andriolo
- Applicant: Mauro Montorsi , Edoardo Mariani , Luca Gambarin , Gianmauro Orru′ , Romeo Scalaprice , Massimo Merlo , Erika Andriolo
- Applicant Address: IT Milan
- Assignee: Newchem S.p.A.
- Current Assignee: Newchem S.p.A.
- Current Assignee Address: IT Milan
- Agency: Silvia Salvadori, P.C.
- Priority: EP10171743 20100803
- International Application: PCT/EP2011/062651 WO 20110722
- International Announcement: WO2012/016860 WO 20120209
- Main IPC: A61K31/34
- IPC: A61K31/34 ; C07D307/94 ; C07J21/00 ; C07J53/00

Abstract:
The invention relates to a process for the preparation of Drospirenone in high yields and purity starting from a compound of formula 2 wherein R is a hydroxyl protective group as defined in the claims, through a sequence of oxidation, deprotection, lactonization and water elimination steps, and wherein the steps of oxidation and lactonization are performed with 1,3,5-trichloro1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (trichloroisocyanuric acid, TCCA) or 1,3-dichloro-1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (dichloroisocyanuric acid, DCCA) or an alkaline metal salt thereof such as the sodium salt dihydrate (DCCA sodium salt) or 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide (IBX). New synthetic intermediates useful for the synthesis of Drospirenone are disclosed, too.
Public/Granted literature
- US20130131335A1 METHODS FOR THE PREPARATION OF DROSPIRENONE AND INTERMEDIATES THEREOF Public/Granted day:2013-05-23
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