Palladium-catalyzed nucleomethylation of alkynes for synthesis of methylated heteroaromatic compounds.

ABSTRACT: Herein, we disclosed a novel and efficient palladium-catalyzed nucleomethylation of alkynes for the simultaneous construction of the heteroaromatic ring and methyl group. The 3-methylindoles, 3-methylbenzofurans and 4-methylisoquinolines were obtained in moderate to excellent yields. Notably, this methodology was employed as a key step for synthesis of a pregnane X receptor antagonist, zindoxifene, bazedoxifene and AFN-1252. The kinetic studies revealed that reductive elimination might be the rate-determining step.

SUBMITTER: Yang X 

PROVIDER: S-EPMC9430495 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature