- 1-(Trifluoromethyl)cyclopent-3-enecarboxylic acid derivatives: Platforms for bifunctional cyclic trifluoromethyl building blocks
-
We report herein the synthesis and applications of 1-(trifluoromethyl) cyclopent-3-ene-1-carboxylic acid and itsesters, promising new trifluoromethylated cyclic building blocks. Initially prepared starting from a pentafluorodithiopropanoic ester, a more convenient and effective approach has been developed starting from commercially available trifluoropropanoic acid or its methyl ester. The interest in these building blocks is exemplified by their use as platforms for a variety of difunctional trifluoromethylcyclopentane derivatives. We disclose herein a promising new building block, 1-(trifluoromethyl)cyclopent-3-enecarboxylic acid (and its esters), accessible in high yield from commercially available trifluoropropanoic acid derivatives. These building blocks exhibit high synthetic potential, given the reaction diversity offered by the double bond and thecarboxylic function. Copyright
- Grellepois, Fabienne,Kikelj, Vincent,Coia, Nicolas,Portella, Charles
-
p. 509 - 517
(2012/03/11)
-
- HETEROCYCLIC CYCLOPENTYL TETRAHYDROISOQUINOLINE AND TETRAHYDROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
-
The present invention is directed to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
- -
-
-