Potential carcinostatics. Synthesis and biological properties of d-and l-. beta.,. beta.-difluoroaspartic acid and. beta.,. beta.-difluoroasparagine

JJM Hageman, MJ Wanner, GJ Koomen…

Index: Hageman; Wanner; Koomen; Pandit Journal of Medicinal Chemistry, 1977 , vol. 20, # 12 p. 1677 - 1679

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Citation Number: 22

Abstract

Di-tert-butyl P, P-difluorooxaloacetate, prepared by fluorination of di-tert-butyl oxaloacetate with perchloryl fluoride, was converted to di-tert-butyl@,@-difluoroaspartate via its 0-methyl oxime, followed by reduction. The tert-butyl ester was hydrolyzed to give a mixture of dl-P, P- difluoroaspartic acid, which was resolved via its brucine salts. dl-Difluoroaspartic acid was converted into P, P-difluoroasparagine by monoesterification and subsequent ...