Bioorganic and Medicinal Chemistry Letters p. 2443 - 2446 (1998)
Update date:2022-08-04
Topics:
Li, Zhengong
Yeo, Su Ling
Pallen, Catherine J.
Ganesan
A library of 108 α,α-difluoromethylenephosphonic acids was prepared by Ugi four-component condensation using Rink-NH2 resin, 4- [(diethoxyphosphinyl)difluoromethyl]benzoic acid, and a set of 18 aldehydes and 6 isonitriles. Following resin cleavage, the diethylphosphonate esters were hydrolyzed with trimethylsilyl bromide to yield the free acids which were assayed for inhibition of PTPα, PTPβ and PTPε.
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