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Synthesis of 4-(5-Benzyl-2-phenylpyrimidin-4-yl)morpholines as Novel PI3K Inhibitors Via Acetates of Baylis-Hillman Adducts and Benzamidines

文献类型：期刊论文

作者Yang, Chunhao2; Yu, Haofei1; Yang, Na2; Meng, Linghua2; Xu, Jing2; Zhang, Rongping1; Xie, Yuyuan2; Ding, Jian2
刊名LETTERS IN ORGANIC CHEMISTRY
出版日期2009-03
卷号6期号:2页码:134-140
关键词Baylis-Hillman adducts PI3K inhibitors pyrimidin-4(3H)-one dihydropyrimidin-4(3H)-one
ISSN号1570-1786
DOI10.2174/157017809787582816
文献子类Article
英文摘要The key intermediates 5-benzyl-2-phenylpyrimidin-4(3H)-ones or ( E)-5-benzylidene-2-phenyl-5,6-dihydropyrimidin-4( 3H)-ones were obtained conveniently by cyclization of the acetates of Baylis-Hillman adducts and benzamidine hydrochloride in the presence of sodium ethoxide at room temperature. Chlorination of pyrimidinones with phosphorus oxychloride and subsequent treatment with morpholine and demethylation yielded PI3K inhibitors.
WOS关键词BIOLOGICAL EVALUATION ; FACILE SYNTHESIS ; DERIVATIVES ; KINASE ; PROTOCOL
资助项目Chinese Academy of Sciences[KSCX2-YW-R-25] ; National Natural Science Foundation of China[20772138] ; National Natural Science Foundation of China[90713034] ; National Natural Science Foundation of China[30721005] ; Science and Technology Commission of Shanghai Municipality Pujiang[08PJ14114] ; Science and Technology Commission of Shanghai Municipality Pujiang[07dz05906]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000263979000007
出版者BENTHAM SCIENCE PUBL LTD
源URL[http://119.78.100.183/handle/2S10ELR8/279304]  
专题药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Yang, Chunhao
作者单位1.Kunming Med Coll, Kunming 650031, Yunnan Province, Peoples R China
2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, SIBS, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Yang, Chunhao,Yu, Haofei,Yang, Na,et al. Synthesis of 4-(5-Benzyl-2-phenylpyrimidin-4-yl)morpholines as Novel PI3K Inhibitors Via Acetates of Baylis-Hillman Adducts and Benzamidines[J]. LETTERS IN ORGANIC CHEMISTRY,2009,6(2):134-140.
APA Yang, Chunhao.,Yu, Haofei.,Yang, Na.,Meng, Linghua.,Xu, Jing.,...&Ding, Jian.(2009).Synthesis of 4-(5-Benzyl-2-phenylpyrimidin-4-yl)morpholines as Novel PI3K Inhibitors Via Acetates of Baylis-Hillman Adducts and Benzamidines.LETTERS IN ORGANIC CHEMISTRY,6(2),134-140.
MLA Yang, Chunhao,et al."Synthesis of 4-(5-Benzyl-2-phenylpyrimidin-4-yl)morpholines as Novel PI3K Inhibitors Via Acetates of Baylis-Hillman Adducts and Benzamidines".LETTERS IN ORGANIC CHEMISTRY 6.2(2009):134-140.

入库方式： OAI收割

来源：上海药物研究所

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