Improved synthesis of the PAR-1 thrombine receptor antagonist RWJ-58259

Autor:	M. Teresa García-López, Rosario Herranz, Ángel M. Valdivielso
Rok vydání:	2009
Předmět:	Indazole Triphosgene medicine.drug_class Organic Chemistry Antagonist Receptor antagonist Combinatorial chemistry lcsh:QD241-441 chemistry.chemical_compound lcsh:Organic chemistry chemistry Yield (chemistry) Reagent Urea medicine Propylene oxide
Zdroj:	ARKIVOC, Vol 2008, Iss 17, Pp 287-294 (2009)
ISSN:	1551-7012
DOI:	10.3998/ark.5550190.0009.h27
Popis:	A significant improvement on the synthesis of the PAR-1 antagonist RWJ-58259 is described, which involves a base-related two-fold yield increase in the indazole N-alkylation, and an easier purification and a nine-fold yield increase in the urea formation, by using triphosgene/propylene oxide as urea coupling traceless reagents.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7499251ed410340954416b30b0d70bc https://doi.org/10.3998/ark.5550190.0009.h27 Zobrazit plný text záznamu