878809-88-2

Upstream product

• 157007-54-0 2-(R)-methylpyrrolidine-1-carboxylic acid tert-butyl ester 
• 75336-86-6 (2R)-methylpiperazine 
• 1765-93-1 4-fluoroboronic acid 
• 878809-59-7 (R)-1-(5-bromo-3-methylpyridin-2-yl)-3-methylpiperazine 
• 833472-84-7 2,4-dichloro-6-(4-fluorophenyl)pyrimidine 
• 117607-13-3 (R)-2-methylpyrrolidine hydrobromide 

Relevant academic research and scientific papers

Development of a Multikilogram Scale Synthesis of a TRPV1 Antagonist

A highly efficient, regioselective five-step synthesis of the TRPV1 antagonist 1 is described. The coupling of piperazine 7 with dichloropyrimidine 8 proceeded via a regioselective Pd-mediated amination affording product 11 in excellent yield. Conversion of the penultimate product 14 afforded 1 through formation of a magnesium ate complex and trapping with CO2.

SUBSTITUTED BIARYL PIPERAZINYL-PYRIDINE ANALOGUES

Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro,and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.