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作为潜在抗基孔肯雅病毒剂的2-亚芳基噻唑并[3,2-]嘧啶的区域选择性汇聚合成。

Regioselective convergent synthesis of 2-arylidene thiazolo[3,2-]pyrimidines as potential anti-chikungunya agents.

作者信息

Fares Mohamed, McCosker Patrick M, Alsherbiny Muhammad A, Willis Anthony C, Clark Timothy, Neyts Johan, Jochmans Dirk, Keller Paul A

机构信息

School of Chemistry & Molecular Bioscience, Molecular Horizons, University of Wollongong, Illawarra Health & Medical Research Institute Wollongong NSW 2522 Australia

School of Chemistry, The University of Sydney NSW 2006 Australia.

出版信息

RSC Adv. 2020 Jan 31;10(9):5191-5195. doi: 10.1039/d0ra00257g. eCollection 2020 Jan 29.

Abstract

Convergent and convenient regioselective synthesis of novel thiazolo[2,3-]pyrimidine derivatives was accomplished using the one-pot reaction of 6-ethylthiouracil, bromoacetic acid, anhydrous sodium acetate, acetic anhydride, acetic acid and suitable aldehyde. X-ray crystallographic study reveals the presence of the configuration of only one regioisomer confirmed by computational studies as being the most likely isomer present.

摘要

通过6-乙基硫脲嘧啶、溴乙酸、无水乙酸钠、乙酸酐、乙酸和合适的醛的一锅法反应,实现了新型噻唑并[2,3 -]嘧啶衍生物的收敛性和便捷的区域选择性合成。X射线晶体学研究表明仅存在一种区域异构体的构型,计算研究证实其为最可能存在的异构体。

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