Process for preparing of bortezomib

US9505787B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9505787-B2
Application numberUS-201314427561-A
CountryUS
Kind codeB2
Filing dateSep 11, 2013
Priority dateSep 11, 2012
Publication dateNov 29, 2016
Grant dateNov 29, 2016

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  1. Title

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  2. Abstract

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  4. Key dates

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  5. First independent claim

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Abstract

Official abstract text for this publication.

The present invention provides improved processes for the preparation of Bortezomib, tert -butyl[1-({(1S)-3-methyl-1-[(3aS,4S,6S,7aS)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl}amino)-1-oxo-3-phenylpropan-2-yl]carbamate of formula (IV) and N-{(1S)-3-methyl-1-[(3aS,4S,6S,7aS)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl} phenylalanine of formula (V). Compound (IV) is prepared by coupling (1R)-3-methyl-1-[(3aS,4S,6S,7aR)-3a,5,5-trimethyl-hexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine of formula (II) or its salt with N-(tert-butoxycarbonyl)-L -phenylalanine of formula (III) in a first solvent in the presence of a first coupling agent and a first base, wherein the coupling process does not comprise solvent exchange. Compound (V) is prepared by deprotecting compound (IV) using an alcoholic solution of an inorganic acid.

First claim

Opening claim text (preview).

The invention claimed is: 1. A process for the preparation of Bortezomib, said process comprising: a) coupling (1R)-3-methyl-1-[(3aS,4S,6S,7aR)-3a5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butan-1-amine of formula (II) or its salt with N-(tert-butoxycarbonyl)-L-phenylalanine of formula (III)…

Assignees

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Classifications

  • Chemistry & Metallurgy · mapped topic

  • Chemistry & Metallurgy · mapped topic

  • C07F5/025Primary

    Chemistry & Metallurgy · mapped topic

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What does patent US9505787B2 cover?
The present invention provides improved processes for the preparation of Bortezomib, tert -butyl[1-({(1S)-3-methyl-1-[(3aS,4S,6S,7aS)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl}amino)-1-oxo-3-phenylpropan-2-yl]carbamate of formula (IV) and N-{(1S)-3-methyl-1-[(3aS,4S,6S,7aS)-3a,5,5-trimethylhexahydro-4,6-methano-1,3,2-benzodioxaborol-2-yl]butyl} phenylalanine of form…
Who is the assignee on this patent?
Cipla Ltd
What technology area does this patent fall under?
Primary CPC classification C07F5/025. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Nov 29 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).