Development of palladium-catalyzed Suzuki carbonylation reaction without external ligand and its application in modification of novel series of α7 nAChR PAMs

doi:10.5246/jcps.2018.07.047

Abstract

Abstract:

Palladium-catalyzed Suzuki carbonylation with CHCl₃ as carbonylative reagent was realized without external ligands. Different substituted benzophenones were explored via the coupling reaction of aryl iodides, arylboronic acids and CHCl₃ as a CO surrogate in moderate to good yields. This method was also successfully applied to the structure modification of α7 nicotinic acetylcholine receptor positive allosteric modulators (α7 nAChR PAMs) based on the preliminary structure-activity relationship.

Key words: Carbonylation reaction, Palladium-catalysis, Benzophenones, CO surrogate

CLC Number:

R916

Supporting:

Ying Meng, Wenxing Zou, Zongze Huang, Xintong Wang, Wenxuan Jiao, Wenjun Xie, Xiling Bian, KeWei Wang, Qi Sun. Development of palladium-catalyzed Suzuki carbonylation reaction without external ligand and its application in modification of novel series of α7 nAChR PAMs[J]. Journal of Chinese Pharmaceutical Sciences, 2018, 27(7): 460-468.

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