The catalytic asymmetric electrophilic functionalization of the less reactive N-heteroaromatic compounds has been reported using the approach of the introduction of an exocyclic amino substituent.
Facile synthesis of fused pyrazolo[1,5-a]dihydropyrimidines and pyrazolo[3,4-b]pyridines is accomplished via intramolecular 6-endo-trig/dig cyclization of 5-aminopyrazoles with 3°/2°-propargylic alcohols and ynones by using p-TSA.
Herein, we achieved a highly efficient enantioselective 1,6-type Friedel–Crafts (hetero)arylation of δ-cyano substituted para-quinone methides with 5-aminopyrazoles.
An efficient asymmetric Friedel–Crafts-type alkylation/cyclization of 5-aminopyrazoles has been developed, affording corresponding pyrazolo[3,4-b]pyridine analogues.
Highly functionalized benzodiazepine skeletons were efficiently synthesized via a Rh(III)-catalyzed selective mono- and dual-C–H bond functionalization/cyclization reaction between readily available 1-aryl-5-aminopyrazoles and iodonium ylides under.