Process for key intermediates for hiv protease inhibitors

Details Process for key intermediates for hiv protease inhibitors Process for key intermediates for hiv protease inhibitors

C - Chemistry, Metallurgy

07

C

C07C 215/28 (2006.01) C07C 213/08 (2006.01) C07C 215/08 (2006.01) C07C 319/20 (2006.01) C07C 323/25 (2006.01)

Patent

CA 2137406

Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of the formula (see formula I) wherein R1 and R2 are amino protective groups and R3 is an amino acid side chain or a protected amino acid side chain. The synthesis involves reacting an aldehyde of the formula Image wherein R1, R2 and R3 are as defined hereinbefore with (chloromethyl)lithium at -20 °C or below and contacting the resulting diastereoisomeric mixture of lithium alcoholates with aqueous hydrochloric acid to obtain a separable mixture of the hydrochloric acid addition salts of the chlorohydrin and its corresponding hydroxy diastereoisomer. The hydrochloric acid addition salt of the chlorohydrin is transformed readily into corresponding optionally amino-protected aminoepoxides; for example, 3(S)- (tert-butyloxycarbonylamino)-1,2(S)-epoxy-4-phenyl- butane.

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