A Process For The Synthesis Of (S) Tetrahydro Alfa (1 Methylethyl) 2 Oxo 1(2 H) Pyrimidineacetic Acid Or Salt Thereof An Intermediate For Antiviral Drugs.

Abstract: A process for preparing (S)-tetrahydro-alfa-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetic acid, an intermediate that is useful in the synthesis of HIV protease inhibitors is described. The process under consideration comprises the following steps: - L-valine is reacted with acrylonitrile and alkyl chloroformate; the N-(2-cyanoethyl)-N-(alkoxycarbonyl)-L-valine thus obtained is hydrogenated on Raney-Nickel catalyst in presence of methanolic ammonia or aqueous ammonia, thus the product resulted was in situ cyclized to give desired compound.

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