Geraldine C. B. Harriman

Synthesis of 4-trifluoromethylpyrido[1,2-a]pyrimidin-2-ones utilizing activated alkynoates

The synthesis of the biologically relevant, 4-trifluoromethylpyrido[1,2-a]pyrimidin-2-one 7, is reported. Addition of substituted 2-aminopyridines 5 to activated alkynoates leads to the facile formation of a series of metabolically stable trifluoromethyl substituted pyrido[1,2-a]pyrimidines under mild conditions.

Selective cell adhesion inhibitors: Barbituric acid based α4β7—MAdCAM inhibitors

A novel series of barbituric acid derivatives were identified as selective inhibitors of alpha4beta7 MAdCAM (mucosal addressin cell adhesion molecule-1) interactions via a high throughput screening exercise. These inhibitors were optimized to submicromolar potencies in whole cell adhesion assays, retaining their selectivity over alpha4beta1 VCAM.

Synthesis of 4-substituted 4-arylpiperidines

Abstract Several novel 4-substituted 4-arylpiperidines were synthesized. The chemistry leading to 4-(4-chlorophenyl)-4-fluoropiperidine ( 6 ), 4-azido-4-(4-chlorophenyl)piperidine ( 7 ) and 4-(4-chlorophenyl)-4-methylpiperidine ( 8 ) is described.