8-[2-Chloro-5-(trifluoromethyl)phenyl]-4H-[1,2,4]oxadiazolo-[3,4-c][1,4]benzoxazin-1-one

8-[2-Chloro-5-(trifluoromethyl)phenyl]-4H-[1,2,4]oxadiazolo-[3,4-c][1,4]benzoxazin-1-one

8-Bromo-4H-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one 1 (NS2028) reacts with [2-chloro-5-(trifluoromethyl)phenyl]boronic acid 2 (2 equiv), Pd(OAc)2 (10 mol%) and KOAc (4 equiv) in acetonitrile heated to ca. 110 °C (sealed tube) for 12 hours to give 8-[2-chloro-5-(trifluoromethyl)phenyl]-4H-[1,2,4...

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Bibliographic Details
Main Authors: Andrey A. Berezin, Panayiotis A. Koutentis
Format: Article
Language:English
Published: MDPI AG 2011-05-01
Series:Molbank
Subjects:
soluble guanylyl cyclase inhibitors
NS2028
benzoxazine
oxadiazole
Suzuki-Miyaura coupling
Online Access:http://www.mdpi.com/1422-8599/2011/2/M728/
Description
Summary:8-Bromo-4H-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one 1 (NS2028) reacts with [2-chloro-5-(trifluoromethyl)phenyl]boronic acid 2 (2 equiv), Pd(OAc)2 (10 mol%) and KOAc (4 equiv) in acetonitrile heated to ca. 110 °C (sealed tube) for 12 hours to give 8-[2-chloro-5-(trifluoromethyl)phenyl]-4H-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one 4 in 64% yield.
ISSN:1422-8599

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