Synthesis 2021; 53(21): 4079-4085
DOI: 10.1055/a-1542-4258
paper

Synthesis of (Hetero)Aryl-Functionalized Azaindoline Derivatives by Palladium-Catalyzed Domino Heck Cyclization/Hiyama Cross-Coupling

Hao Ye
a   College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, P. R. of China
,
Ruotong Zhang
a   College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, P. R. of China
,
Xiaolong Xia
b   School of Textile and Clothing, Nantong University, Nantong 226019, P. R. of China
,
Yue Ding
a   College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, P. R. of China
c   Anhui Haifeng Analysis and Testing Technology Co. Ltd, Hefei 230000, P. R. of China
,
Meihui Sun
a   College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, P. R. of China
c   Anhui Haifeng Analysis and Testing Technology Co. Ltd, Hefei 230000, P. R. of China
,
Lei Shi
a   College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, P. R. of China
,
Guomin Jiang
a   College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, P. R. of China
,
Xin-Xing Wu
a   College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, P. R. of China
› Author Affiliations
The generous financial support from the Program of High-Level Talents of Nantong University (03083031) is gratefully acknowledged.


Abstract

A palladium-catalyzed domino Heck cyclization/Hiyama cross-coupling has been achieved for the synthesis of (hetero)aryl-functionalized azaindoline derivatives bearing all-carbon quaternary centers in 46–85% yields. The synthetic versatility of this protocol has been highlighted by the gram-scale synthesis and modification of aryl-containing complex bioactive molecules.

Supporting Information



Publication History

Received: 24 May 2021

Accepted after revision: 01 July 2021

Accepted Manuscript online:
01 July 2021

Article published online:
22 July 2021

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