A Convenient Preparation of Tetrahydropteridines and Tetrahydrofolate Analogs. Synthesis of Tetrahydro-3′,5′-Dichloromethotrexate

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Abstract
Tetrahydropteridine enzymatic cofactors and inhibitors [some of which are used in cancer chemotherapy] may be conveniently prepared by reduction of the aromatic precursors with dimethylamine-borane in glacial acetic acid. A short reaction time at 20-60.degree. C affords tetrahydrofolate analogs in high yield and purity under anhydrous conditions and without protection from air. 3'',5''-Dichloromethotrexate is reduced without hydrogenolysis of Cl.

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