L. Haitao
2011
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Journal
Chinese Journal of Pharmaceuticals
Abstract
R-Methotrexate was synthesized from 4-(methylamino) benzoic acid by carbobenzyloxy protection, amidization with diethyl D-glutamate hydrochloride,catalytic hydrogenolysis and then hydrolysis to give N-(4- methylaminobenzoyl) -D-glutamic acid,which was subjected to one-pot simultaneous reaction with 2,4,5,6-tetraamnio-pyrimidine sulfate and 1,1,3-tribromoacetone with an overall yield of about 23%.