Synthesis 2023; 55(09): 1419-1426
DOI: 10.1055/a-1996-8388
paper

TBHP/KI-Promoted Oxidative Cyclization of α-Aminoketones for One-Pot Synthesis of Substituted 2-Acyloxazoles

Jiecheng Zheng
a   Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, P. R. of China
,
Dali Zhu
a   Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, P. R. of China
,
Zhangyou Yang
a   Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, P. R. of China
,
Huali Chen
a   Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, P. R. of China
,
Wei Wang
b   Chongqing Fuling Institute for Food and Drug Control, Chongqing 408102, P. R. of China
,
Lin Ling Gan
c   Chongqing Engineering Research Center of Pharmaceutical Sciences, School of Pharmacy, Chongqing Medical and Pharmaceutical College, Chongqing 401331, P. R. of China
,
Zongjie Gan
a   Department of Medicinal Chemistry, College of Pharmacy, Chongqing Medical University, Chongqing 400016, P. R. of China
› Author Affiliations
We appreciate the finical support from the National Natural Science Foundation of China (No. 21907013).


Abstract

A metal-free and facile synthesis of substituted 2-acyloxazole derivatives from α-aminoketones was developed via a TBHP/KI-promoted oxidative cyclization. This procedure proceeded smoothly under mild conditions and a broad scope of 2-acyloxazoles were obtained in moderate to good yields.

Supporting Information



Publication History

Received: 14 October 2022

Accepted after revision: 12 December 2022

Accepted Manuscript online:
12 December 2022

Article published online:
05 January 2023

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