It is the principal intermediate field for the HIV protease inhibiters, reflected image purity (s and s) the production method of minding, those chlorhydrin of amino epoxides

摘要

(57) Abstract Formula (1) (R¹ and R² is the amino protective group, as for R^{3 the} amino acid side chain or the amino acid side chain which is protected is) large-scale production of hydrochloric acid attaching salting of chlorhydrin discloses possible three-dimensional unique synthetic method. Formula (2) (R¹, as for R² and R³ above-mentioned ones is in the synthetic method) aldehyde (chloromethyl) the process which reacts lithium at temperature below the 20, and making with jiasutereoisoma and water hydrochloric acid contact of the lithium alcoholate which is obtained, hydrochloric acid attaching salting of chlorhydrin and that the process which obtains the separated possible blend of hidorokishijiasutereoisoma which corresponds is included. Hydrochloric acid attaching salting of chlorhydrin corresponds, easily, optionally amino - the amino epoxide which is protected, for example, 3 (S) - (tert butyl oxy carbonyl amino) 1,2 (S) it is possible to make - epoxy 4 phenyl - butane.