Über Pterinchemie. 54. Mitteilung [1]. Eine allgemeine Methode zur Synthese von Folsäure, Folsäurekonjugaten und Folsäureanalogen

Abstract

A general method for synthesis of folic acid, its conjugates and analogues . A new and general method for the synthesis of folic acid, folic acid conjugates and folic acid analogues is described. The key step, i.e. the condensation of N(2′)‐acetyl‐6‐formyl‐pterine (I: R 1  COCH 3 ) with aminoaryl derivatives II, is achieved by refluxing in absolute ethanol to afford the azomethines III. NaBH 4 ‐reduction followed by basic hydrolysis gives pure V products in high yield, free from 7‐isomers.