The Synthesis of the 3'-Fluoro and 3', 5'-Difluoro Derivatives of 4-Amino-4-deoxy-N10-methylpteroylglutamic Acid (Methotrexate) 1

AS TOMCUFCIK, DR SEEGER

Index: Tomcufcik,A.S.; Seeger,D.R. Journal of Organic Chemistry, 1961 , vol. 26, p. 3351 - 3356

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Citation Number: 12

Abstract

IV. c1 H highly effective in prolonging the life span of mice with advanced leukemia (L1210). 3 In our laboratories, these compounds have been found to inhibit the growth of the transplanted 6C3HED mouse lymphosar~ oma.~ It was thus of interest to prepare the corresponding 3'-fluoro (11) and 3', 5'-difluoro (111) derivatives of methotrexate (I) for evaluation as antineoplastic agents. Since the direct introduction of fluorine into the ...