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一种由羧酸、氨基酸和硼酸合成2,4,5-三取代恶唑方法的开发。

Development of a method for the synthesis of 2,4,5-trisubstituted oxazoles composed of carboxylic acid, amino acid, and boronic acid.

作者信息

Yamada Kohei, Kamimura Naoto, Kunishima Munetaka

机构信息

Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical, and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.

出版信息

Beilstein J Org Chem. 2017 Jul 27;13:1478-1485. doi: 10.3762/bjoc.13.146. eCollection 2017.

Abstract

A novel method for the synthesis of trisubstituted oxazoles via a one-pot oxazole synthesis/Suzuki-Miyaura coupling sequence has been developed. One-pot formation of 5-(triazinyloxy)oxazoles using carboxylic acids, amino acids and a dehydrative condensing reagent, DMT-MM, followed by Ni-catalyzed Suzuki-Miyaura coupling with boronic acids provided the corresponding 2,4,5-trisubstituted oxazoles in good yields.

摘要

一种通过一锅法恶唑合成/铃木-宫浦偶联序列合成三取代恶唑的新方法已被开发出来。使用羧酸、氨基酸和脱水缩合试剂DMT-MM一锅法形成5-(三嗪基氧基)恶唑,然后与硼酸进行镍催化的铃木-宫浦偶联,以良好的产率得到相应的2,4,5-三取代恶唑。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7f78/5550800/5c51e3251ae3/Beilstein_J_Org_Chem-13-1478-g002.jpg

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