Invention Grant
US08481751B2 Process for the production of bendamustine alkyl ester, bendamustine, and derivatives thereof
有权
苯达莫司汀烷基酯,苯达莫司汀及其衍生物的生产方法
- Patent Title: Process for the production of bendamustine alkyl ester, bendamustine, and derivatives thereof
- Patent Title (中): 苯达莫司汀烷基酯,苯达莫司汀及其衍生物的生产方法
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Application No.: US13334402Application Date: 2011-12-22
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Publication No.: US08481751B2Publication Date: 2013-07-09
- Inventor: Kai Groh , Holger Rauter , Dirk Born
- Applicant: Kai Groh , Holger Rauter , Dirk Born
- Applicant Address: DE Hanau
- Assignee: Heraeus Precious Metals GmbH & Co. KG
- Current Assignee: Heraeus Precious Metals GmbH & Co. KG
- Current Assignee Address: DE Hanau
- Agency: Panitch Schwarze Belisario & Nadel LLP
- Priority: DE102010055499 20101222
- Main IPC: C07D235/12
- IPC: C07D235/12

Abstract:
Methods are provided for the production of bendamustine alkyl ester, bendamustine, as well as derivatives thereof. With the methods the production of these compounds is possible in reproducibly high yields. To this end, hydroxyl-group-containing esters are used as the starting material, whose hydroxyl groups are substituted in a simple way by halogen groups. This substitution is possible in the presence of (i) oxalyl chloride and (ii) dialkylformamide, dialkyl acetamide or dimethyl sulfoxide. In a subsequent reaction, the resulting esters can be hydrolyzed to form the acid.
Public/Granted literature
- US20120165543A1 PROCESS FOR THE PRODUCTION OF BENDAMUSTINE ALKYL ESTER, BENDAMUSTINE, AND DERIVATIVES THEREOF Public/Granted day:2012-06-28
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