Synthesis and biological properties of 3??methyl??10??propargyl??5, 8??dideazafolic acid

TR Jones, RF Betteridge, DR Newell…

Index: Jones; Betteridge; Newell; Jackman Journal of Heterocyclic Chemistry, 1989 , vol. 26, # 5 p. 1501 - 1507

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Citation Number: 6

Abstract

Abstract The synthesis of N 3-methyl-10-propargyl-5, 8-dideazafolic acid (1b) is described. Ring closure of methyl-5-methylanthranilate with chloroformamidine hydrochloride gave a high yield of pure 2-amino-4-hydroxy-6-methylquinazoline treatment of which with iodomethane/sodium hydroxide provided the corresponding 3-methylquinazoline (6) which was converted to its 2-pivaloylamino derivative. This synthetic approach, next involving ...