Process for making HIV protease inhibitors

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

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544388, 544390, C07D40106

Patent

active

056124848

ABSTRACT:
A process for making a clinically efficacious HIV protease inhibitor Compound J eliminates one step in its synthesis, by an improved, alternative synthesis of the 2(S)-4-picolyl-2-piperazine-t-butyl-carboxamide intermediate.

REFERENCES:
Giraud-Clenet, et al., Compt. Rend., t. 262, pp. 224-227, 1966.
Krimen, et al., "The Ritter Reaction", Organic Reactions, vol. 17, pp. 213-325, 1969.
Mowry, et al., "The Preparation of Nitriles", Chem. Rev., 42, pp. 189-283, 1947.
Ugi, et al., "The Passerini and Ugi Reactions", Comprehensive Organic Synthesis, vol. 4, pp. 1083-1109, 1991.

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