Solid-phase synthesis of potential protein tyrosine phosphatase inhibitors via the Ugi four-component condensation

DOI: 10.1016/S0960-894X(98)00408-9

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2443 - 2446 (1998)

Update date:2022-08-04

Topics:

Authors:

Li, Zhengong

Yeo, Su Ling

Pallen, Catherine J.

Ganesan Ganesan

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Article abstract of DOI:10.1016/S0960-894X(98)00408-9

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.

Full text of DOI:10.1016/S0960-894X(98)00408-9

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