A synthetic approach to poly (. gamma.-glutamyl) conjugates of methotrexate

…, GS McCaleb, JA Montgomery

Index: Piper, James R.; McCaleb, George S.; Montgomery, John A. Journal of Medicinal Chemistry, 1983 , vol. 26, # 2 p. 291 - 294

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Citation Number: 21

Abstract

Methotrexate poly (yi-g1utamate) s bearing two and three glutamate units above that present in methotrexate have been synthesized by extension of a previously described route used to synthesize the lower conjugate bearing one added glutamate unit. Key steps in the sequence are the peptide coupling of N-[4-[[(benzyloxy) carbonyl]-methylamino] benzoyl]-L- glutamic acid a-benzyl ester (5) with oligo (yL-glutamate) benzyl esters, removal of ...