Tetrahydrofuran → 6-Chloro-2-(3-chloropyridin-4-yl)-5-(trifluoromethyl)benzoxazole

To a mixture of 0.46 g of 3-chloro-N-[4-chloro-2-hydroxy-5-(trifluoromethyl)phenyl]isonicotinamide, 5 ml of tetrahydrofuran and 0.38 g of triphenylphosphine, 0.63 g of 40% toluene solution of diethyl azodicarboxylate was added dropwise at room temperature, and the reaction mixture was stirred for two hours. The reaction mixture was concentrated under reduced pressure. The residue was subjected to silica gel column chromatography to give 0.39 g of 6-chloro-2-(3-chloropyridin-4-yl)-5-(trifluoromethyl)benzoxazole (hereinafter, referred to as “active compound 81”).

1. additionwas added dropwise at room temperature
2. concentrationThe reaction mixture was concentrated under reduced pressure

ORD-Eintrag

ord-e1458eb80e2d4054be36f5b344921ea3

Quelldatensatz

uspto-grants-2012_08

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US08242133B2