| abstract |
PURPOSE: To produce the titled compound useful as an immunoactivator and analgesic agent, easily, in high yield, by condensing an α-amino acid derivative with a malonic acid diester alkali metal salt, and removing the protecting group from the product. n CONSTITUTION: The objective compound of formula IV (the steric configuration of the C atom labeled with * is R, S or its combination) can be produced by (1) condensing (A) the α-amino acid derivative of formula I (R 1 is α-amino acid residue, etc. corresponding to the α-amino acid molecule minus α-carboxyl group; X is Br or I) with (B) the substituted or unsubstituted malonic acid diester alkali metal salt of formula II (R 2 is H, 1W6C alkyl, etc.; R 3 is 1W4C alkyl or carboxyl-protecting group; Me is alkali metal) in an organic solvent such as formamide at 0W15°C, and (2) removing the protecting group from the reaction product by conventional decarboxyl reaction or decarboxylate reaction. n COPYRIGHT: (C)1985,JPO&Japio |