✦ LIBER ✦

Synthesis of 14C-methotrexate: (N-[p-[[2,4-diamino-4-deoxy-6-pteridinyl]methyl]methylamino]-benzoyl) -L-14C-glutamic acid

✍ Scribed by M. G. Nair; Charles M. Baugh

Publisher: John Wiley and Sons
Year: 1977
Tongue: French
Weight: 270 KB
Volume: 13
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580130116

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✦ Synopsis

Abstract

A simple and general method for the synthesis of folate analogs labeled in the glutamate moiety with ^14^C is described. The synthesis makes use of the trimethylsilyl derivative of L‐glutamic acid 8 for the coupling reaction with the activated pteroate analogs. Deprotection under mild conditions circumvented the potential problems associated with deamination at the 4‐position of 2. Methotrexate, folic acid, and N^10^ ‐ methyl folic acid were prepared in ˜50% yield by the use of this procedure.

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