| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain in high stereo-selectivity the subject compound which is a raw material for manufacture of an HIV protease inhibitor, by carrying out a reaction of a cyanohydrin derivatives with a 2-amino-3-phenylpropanal derivative in the presence of a metal compound, a base or an acid catalyst. SOLUTION: The objective compound of formula III is obtained by carrying out the reaction of an aminoaldehyde derivative of formula I (R<1> and R<2> are each H, a protecting group of amino group) with a cyanohidrin derivatives of formula II (R<3> and R<4> are each an alkyl group, etc.) in the presence of a metal compound such as trimethylaluminum, etc., the base such as triethylamine, sodium hydroxide, etc., the acid such as hydrochloric acid, sulfuric acid, etc. For example 1.0-10 equivalent acetonecyanohydrin is added to the compound of formula I, 0.1-10 equivalent metal compound as the reaction promoter is added to the compound of formula I, and a solvent which does not react with the raw materials is preferred as the reaction solvent, and preferably the reaction is carried out at -100 deg.C to the boiling temperature of the reaction solvent preferably using ethylene-chloride.</p> |
