Invention Grant
- Patent Title: Process for the preparation of boronic acid esters
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Application No.: US16484346Application Date: 2018-02-19
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Publication No.: US11667654B2Publication Date: 2023-06-06
- Inventor: Maneesh Kumar Pandey , Raj Narayan Tiwari , Sonu Shukla , Sarbjot Singh Sokhi , Govind Singh , Saswata Lahiri , Walter Cabri
- Applicant: FRESENIUS KABI ONCOLOGY LIMITED
- Applicant Address: IN New Delhi
- Assignee: Fresenius Kabi Oncology Ltd.
- Current Assignee: Fresenius Kabi Oncology Ltd.
- Current Assignee Address: IN New Delhi
- Agency: Leydig, Voit & Mayer, Ltd.
- Priority: IN 1711005668 2017.02.17
- International Application: PCT/IB2018/050999 2018.02.19
- International Announcement: WO2018/150386A 2018.08.23
- Date entered country: 2019-08-07
- Main IPC: C07F5/02
- IPC: C07F5/02

Abstract:
The present invention relates to an improved process for the preparation of a compound of formula (I), wherein PG1 may be independently selected from tert-butyloxycarbonyl (Boc), phthaloyl, 9-fluorenylmethyloxycarbonyl (Fmoc), triphenylmethyl (Trityl), carboxybenzyl (Cbz), trifluoroacetyl, benzyl (Bn), benzylidene, methanesulfonyl (Mesyl), toluene sulfonyl (Tosyl) or acyl; its isolation as solid and use for the preparation of the compound of formula (IV), in particular the compound of formula (IV) i.e. [(1R)-3-methyl-1[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl) amino]propyl]amino]butyl] boronic acid with more than 99.95% chiral purity, as measured by HPLC.
Public/Granted literature
- US20200031850A1 AN IMPROVED PROCESS FOR THE PREPARATION OF BORONIC ACID ESTERS Public/Granted day:2020-01-30
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