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Potential carcinostatics V. Synthesis and properties of potential inhibitors of the adenylosuccinate synthetase and adenylosuccinate lyase system

✍ Scribed by M. J. Wanner; E. M. van Wijk; G. J. Koomen; U. K. Pandit

Book ID
104588190
Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
443 KB
Volume
99
Category
Article
ISSN
0165-0513

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✦ Synopsis

Abstract

β,β‐Dimethylaspartic acid was obtained by the aluminium‐amalgam reduction of the O‐methyloxime of diethyl 2‐oxo‐3,3‐dimethyl‐1,4‐butanedioate and subsequent hydrolysis. The (latter) diester was conveniently prepared by the condensation of ethyl 2‐bromo‐2‐methylpropionate with diethyl oxalate, under the influence of magnesium. β,β‐Difluoroaspartic acid, threo β‐methylaspartic acid and β,β‐dimethylaspartic acid (as racemates) were coupled with 6‐chloropurin‐9‐yl riboside to yield the corresponding nucleosides. The bases methyl 7‐oxo‐7__H__‐pyrido[2.1‐i]purine‐9‐carboxylate and 6‐[2,3‐bis(methoxycarbonyl)propyl]purine were converted into the corresponding nucleosides by coupling with O^2^,O^3^,O^5^‐tribenzoylribofuranosyl chloride and removal of the protecting groups. The biological test results on leukemia P‐388 are presented.

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