Process for obtaining valine derivatives useful for obtaining a pharmaceutically active compound
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United States of America Patent
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Jun 21, 2011
Grant Date -
Sep 23, 2010
app pub date -
Oct 19, 2006
filing date -
Oct 20, 2005
priority date (Note) -
Expired
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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.
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