Solid phase synthesis of arylretinamides

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

Reexamination Certificate

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C554S060000

Reexamination Certificate

active

07550510

ABSTRACT:
A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.

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Abstract, “Solid-phase assisted synthesis of a library of N-(4-hydroxyphenyl)retinamide (4-HPR) analogs” By Mershon, et al., Aug. 2001 American Chemical Society Meeting.
Abstract, “Solid Phase-Assisted Synthesis and Screening of a Library of N-(4-Hydroxypheny)Retinamide Analogs” by Mershon, et al., Jun. 2002 FASEB Summer Research Conference.
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