(2S,3S,5S)-2,5-Diamino-3-hydroxy-1,6-diphenylhexane, the key intermediate of lopinavir was synthesized from L-phenylalanine by N,O-benzylation, cyanidation, Grignard reaction and reduction to give (2S,3S,5S)-5-amino-2-dibenzylamino-1,6-diphenylhexan-3-ol, which was subjected to debenzylation with an overall yield of about 63%.

This study successfully synthesized (2S,3S,5S)-2,5-Diamino-3-hydroxy-1,6-diphenylhexane, a key intermediate in lopinavir, from L-phenylalanine with a yield of 63%.

Paper

Synthesis of (2S,3S,5S)-2,5-Diamino-3-hydroxy-1,6-diphenylhexane

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