Rh(III)-catalyzed C-H activation/intramolecular annulation for the synthesis of N-methoxydihydropyrimidin-2-one fused heterocycles

被引:1
作者
Huang, Youchun [1 ]
Kang, Ke [1 ]
Zhong, Xiuwen [1 ]
Yu, Yongping [1 ]
Chen, Wenteng [1 ]
机构
[1] Zhejiang Univ, Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China
关键词
C -H activation; Intramolecular annulation; Rh(III)-catalyzed; N-Methoxydihydropyrimidin-2-one; CHEMODIVERGENT ANNULATIONS; REVERSE-TRANSCRIPTASE; SULFOXONIUM YLIDES; INHIBITION; ACTIVATION; INDOLES;
D O I
10.1016/j.tetlet.2022.154311
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A facile rhodium-catalyzed C-H activation/intramolecular annulation strategy for N-methoxydihydropyrimidin-2-one was well realized in water media. Moreover, this Rh(III)-catalytic system facilitated the construction of N-methoxydihydropyrimidin-2-one scaffolds reminiscent of unnatural amino alcohols, transformation to pyran-2-one fused heterocycles as well as late-stage modification of drug molecules. Also, the protocol was easily scaled up to a gram-scale level. And H2O was proposed to act as an alternative coordination molecule to accelerate the generation of active Rh(III) catalyst species. (c) 2022 Elsevier Ltd. All rights reserved.
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页数:6
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