| 摘要 |
<p>PURPOSE:To obtain the titled compound having an inhibiting action on aminopeptidase B in high yield, by reacting N-protecting 2-oxoethylamine with glyoxylic acid or its ester, reducing the reaction product, followed by condensing the reduced compound with an aminoacetic acid. CONSTITUTION:A compound [e.g., N-[2-oxo-2-(4'-chlorophenyl)] acetamide, etc.] shown by the formula I (R1 is naphthyl, etc.; R2 is protected amino) is reacted with a compound shown by the formula II (R3 is H or ester residue) or its ester (e.g., glyoxylic acid, etc.). The prepared compound is reduced, and, if necessary, after the process of the removal of ester residue, optical resolution and/or removal of the amino-pretecting group, to give a compound shown by the formula III (R2' is amino or protected amino). A compound shown by the formulaIV(R4 is 3-4C alkyl, etc.), after protecting a group which will not participate in the reaction of the compounds shown by the formulas III and IV, is condensed with the compound shown by the formula III, and the protecting group is removed to give a compound shown by the formula V.</p> |
