ChemInform Abstract: Synthesis of New Isoxazoles from Isoxazo‐Chalcones, Chalcone Dibromides, Epoxides and Acetylated Ketoximes.

Abstract

Die aus den Chalkonen (I) mit NH2OH (II) erhaltenen Isoxazoline (III) werden thermisch zu den Isoxazolen (IV) dehydriert oder lassen sich auch direkt aus (I) und (II) in Essigsäure darstellen.

Discovery of an Orally Active Series of Isoxazoline Glycoprotein IIb/IIIa Antagonists

“…3-[[[3-[4-(Aminoiminomethyl)phenyl]-5-isoxazolyl]acetyl]amino]- N -(butoxycarbonyl)- l - alanine Trifluoroacetate (27). To a suspension of 28 (5.28 g, 21.62 mmol) in CHCl 3 (150 mL) was added NBS (4.23 g, 23.78 mmol) and AIBN (100 mg), and the mixture was warmed to reflux …”

“…To a suspension of 28 (5.28 g, 21.62 mmol) in CHCl 3 (150 mL) was added NBS (4.23 g, 23.78 mmol) and AIBN (100 mg), and the mixture was warmed to reflux. 54 A small amount of AIBN (100-200 mg) was added at 1 h intervals until TLC indicated a complete reaction. Potassium acetate (17.3 g) and HOAc (6.5 mL) were added, and the reaction mixture was heated at reflux for 1 h, cooled, and then poured into 1 N NaOH (325 mL).…”