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Rhodium(III)‐Catalyzed Alkynylation of 4‐Arylphthalazin‐1(2 H )‐one Scaffolds via C‐H Bond Activation
Author(s) -
Du Xuxin,
Hou Hongcen,
Zhao Yongli,
Sheng Shouri,
Chen Junmin
Publication year - 2020
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201901731
Subject(s) - alkynylation , chemistry , rhodium , catalysis , aryl , functional group , combinatorial chemistry , substrate (aquarium) , molecule , salt (chemistry) , annulation , stereochemistry , medicinal chemistry , organic chemistry , alkyl , oceanography , geology , polymer
Selective C–H bond alkynylation toward modular access to material and pharmaceutical molecules is of great desire in modern organic synthesis. Disclosed herein is rhodium(III)‐catalyzed selective C–H bond mono‐/bialkynylation of 4‐aryl phthalazin‐1(2 H )‐one was developed. The silver salt AgSbF 6 are demonstrated to play a vital role in promoting the bialkynylation reactions. The present alkynylation strategy is simple, efficient, and features high functional group tolerance and broad substrate scope under an air atmosphere. Additionally, 6‐aryl pyridazin‐3(2 H )‐one scaffold is amenable to the selective monoalkynylation and sequential bialkynylation, respectively.