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Jun-Ke Wang, Ying-Xiao Zong, Xi-Cun Wang, Yu-Lai Hu, Guo-Ren Yue.Synthesis of?N-benzothiazol-2-yl-amides by Pd-catalyzed C(sp2)-H functionalization[J]. CCL, 2015,26(11): 1376-1380??Synthesis of?N-benzothiazol-2-yl-amides by Pd-catalyzed C(sp2)-H functionalizationJun-Ke Wanga,b,c, Ying-Xiao Zonga,b, Xi-Cun Wanga,b?, Yu-Lai Hua,b?, Guo-Ren Yuea????a?Key Laboratory of Hexi Corridor Resources Utilization of Gansu Universities, College of Chemistry and Chemical Engineering, Hexi University, Zhangye 734000, China;b?Gansu Key Laboratory of Polymer Materials, College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou 730070, China;c?Gansu Engineering Laboratory of Applied Mycology, Hexi University, Zhangye 734000, ChinaReceived 11 May 2015, Received in revised form 29 June 2015, Accepted 1 July 2015,Available online 10 August 2015.E-mail addresses: wangxicun@;huyulai@126.comAbstract: A catalytic synthesis of?N-benzothiazol-2-yl-amides from 1-acyl-3-(phenyl)thioureas was achieved in the presence of a palladium catalyst through the C(sp2)-H functionalization/C-S bond formation. This synthetic methodology can produce various?N-benzothiazol-2-yl-amides in high yields with good functional group tolerance.Key words:?Benzothiazole?????Pd-catalyzed?????1-Acyl-3-phenylthiourea?????C-H functionalization?????L-Proline????1. IntroductionThe benzothiazole moiety is an important scaffold due to its widespread occurrence in bioactive natural products,pharmaceuticals, organic optoelectronic materials,and ligands for phosphorescent complexes [1-4]. In particular,substituted Nbenzothiazol- 2-yl-amides are an important class of heterocyclic compounds that exhibit a wide range of biological properties [5-9] such as ubiquitin ligase inhibition?[5],antitumor?[6],antirotavirus infections?[7],modulating the adenosine receptor?[8,?9],and the nuclear hormone receptor?[9]. For example,the?N-benzothiazol-2- yl-cyclohexanecarboxamide,as a new anticancer drug,was selected as one