| 摘要 |
<p>PROBLEM TO BE SOLVED: To realize an industrially short-cut process for producing 3-amino-2- oxo-1-hydroxypropane derivative in high yield, from a compound obtained by anα-amino acid via a novel intermediate to this derivative which is important as an intermediate for a variety of HIV protease inhibitors. SOLUTION: A compound of formula (Rs are H, an alkyl, an aryl, an aralkyl; P1 and P2 are H, amino-protecting group; E1 is phenoxy, benzyloxy) is allowed to react with an alkali metal enolate derived from a glycolic ester of formula II (R1 is an alkyl, an aryl; R2 is H, an alkyl, aryl) to give a new compound of formula III, 4-amino-3-oxo-2-hydroxybutanoic ester derivative, followed by hydrolysis of the ester group and decarboxylation to give an optically active 3-substituted-3-amino-1,2-epoxypropane derivative as an equivalent ofα- aminoalcohol derivative which is important as an intermediate for HIV protease inhibitor or a kind of enzyme inhibitor.</p> |
