Site‐Selective Direct Arylation of 1,2,3‐Triazole N‐Oxides

Abstract

An efficient route for the synthesis of 2,4-disubstituted 1,2,3triazoles by the regioselective direct arylation of 2-aryl-1,2,3triazole N-oxides with Ar-X [X = Br, I and B(OH) 2 ] is demon-

New Arylating Agents in Pd-Catalyzed C–H Bond Functionalization of 5-Membered Ring Heteroarenes

“…A slightly simpler procedure was reported in 2011 for the arylation of benzoxazoles and benzothiazoles [24]. In 2013, Kuang et al reported the Pd(OAc) 2 -catalyzed synthesis of 3,4-diarylsydnones and of 5-aryltriazoles by coupling with arylboronic acids [25,26].…”

Five-Membered Hetarene N-Oxides: Recent Advances in Synthesis and Reactivity

“…The scope of CH-functionalization of 1,2,3-triazole 1-oxides 33 was also expanded on other coupling partners including boronic acids, 35 aryl halides 36 and sulfonates. 37 All three synthetic protocols proceeded efficiently under Pd(OAc)2 catalysis with good and high yields of target products 38 and high C(5) regioselectivity (Scheme 12).…”

“…It should be noted that the developed conditions were suitable for the homocoupling of several other representative hetarene Noxides. 34 The scope of the CH-functionalization of 1,2,3-triazole 1-oxides 33 was also expanded by using other coupling partners including boronic acids, 35 aryl halides 36 and sulfonates. 37 All three synthetic protocols proceeded efficiently under Pd(OAc) 2 catalysis, with good to high yields of the target products 38 and high C(5) regioselectivity being obtained (Scheme 12).…”