Improved loading and cleavage methods for solid-phase synthesis using chlorotrityl resins: synthesis and testing of a library of 144 discrete chemicals as potential farnesyltransferase inhibitors.

Published

Journal Article

The use of chlorotrityl resins for the immobilization of amines is sometimes deterred by the lengthy process of loading the reactants on the resins and product decomposition caused by the reactive chlorotrityl group in the presence of 1% TFA as a cleavage agent. Here, we report improved methods developed for selective and efficient loading of aminobenzoic acid derivatives on chlorotrityl resins and for cleavage of aniline-containing products from the resins without decomposition. These methods led to the synthesis of a library of 144 discrete chemicals as potential farnesyltransferase inhibitors (FTIs) using IRORI's radio-frequency-encoded sorting technique and to the study of the applicability of the bivalence approach to the development of FTIs.

Full Text

Duke Authors

Cited Authors

  • Park, JG; Langenwalter, KJ; Weinbaum, CA; Casey, PJ; Pang, Y-P

Published Date

  • May 2004

Published In

Volume / Issue

  • 6 / 3

Start / End Page

  • 407 - 413

PubMed ID

  • 15132601

Pubmed Central ID

  • 15132601

Electronic International Standard Serial Number (EISSN)

  • 1520-4774

International Standard Serial Number (ISSN)

  • 1520-4766

Digital Object Identifier (DOI)

  • 10.1021/cc0340729

Language

  • eng