Process for producing optically active amides

摘要

The present invention provides an industrial process for producing decahydro (4aS,8aS)isoquinoline-3(S)-carboxamides(4; R=H or C1-6 alkyl) which are useful as intermediates of Saquinavir (EP432694) that has been proposed as an anti-AIDS agent. Tetrahydroisoquinoline-3(S)-carboxylic acid (1) is reacted with at least one of phosgene, phosgene dimer and triphosgene to form N-carboxy anhydride (NCA) (2). This is reacted with an amine to produce a tetrahydroisoquinoline-3(S)-carboxamide derivative (3), which can be reduced in the presence of a metal catalyst (preferably Ru) to produce (4). <CHEM> <CHEM>