Volume 22, Issue 39
Heterocyclic Compounds
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ChemInform Abstract: First Use of the Taylor Pteridine Synthesis as a Route to Polyglutamate Derivatives of Antifolates.

H. BADER

H. BADER

Dana-Farber Cancer Inst., Dep. Biol. Chem. Mol. Pharm., Harvard Med. School, Boston, MA 02115, USA

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A. ROSOWSKY

A. ROSOWSKY

Dana-Farber Cancer Inst., Dep. Biol. Chem. Mol. Pharm., Harvard Med. School, Boston, MA 02115, USA

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First published: October 1, 1991

Abstract

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ChemInform Abstract

Starting with the condensation reaction between the nitrobenzoyl derivative (I) of L-glutamate and di-tert-butyl L-glutamate (II), the pyrazine-substituted diglutamate (VI) is prepared. This reacts with acetamidine acetate (VII), performing a Taylor pteridine synthesis to give the tri-tert-butyl derivative (VIII) of 2-deamino-2- methylaminopterin diglutamate.

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