Method of making pteridine compounds

摘要

A method for the preparation of pteridine compounds such as methotrexate is disclosed. 2,4-diamino-6-pteridine-methanolxHBr is reacted with triphenylphosphine dibromide or phosphorus tribromide to form 6-(bromomethyl)-2,4-diamino-pteridine hydrobromide and the bromine atom in the molecule is then replaced with the functional group, N-[4-(methylamino)-benzoyl]-L-glutamic acid in the case of methotrexate and N-(4-aminobenzoyl)-L-glutamic acid in the case of aminopterin.