Process for obtaining valine derivatives useful for...

Details Process for obtaining valine derivatives useful for... Process for obtaining valine derivatives useful for...

2011-06-21

2011-06-21

Powers, Fiona T (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Sulfonate esters

C558S054000, C558S056000, C562S567000

Reexamination Certificate

active

07964749

ABSTRACT:
The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an —OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a “one pot” reaction.

REFERENCES:
patent: 7439261 (2008-10-01), Verardo et al.
patent: 7728021 (2010-06-01), Dalmases Barjoan et al.
patent: 2009/0124577 (2009-05-01), Rafecas Jane et al.
patent: WO 2004/026847 (2004-04-01), None

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