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

doi:10.2174/157017809787582816

	Synthesis of 4-(5-Benzyl-2-phenylpyrimidin-4-yl)morpholines as Novel PI3K Inhibitors Via Acetates of Baylis-Hillman Adducts and Benzamidines
	Yang, Chunhao2 ; Yu, Haofei 1; Yang, Na 2; Meng, Linghua2 ; Xu, Jing 2; Zhang, Rongping 1; Xie, Yuyuan2 ; Ding, Jian2
刊名	LETTERS IN ORGANIC CHEMISTRY
	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
DOI	10.2174/157017809787582816
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.
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关键词	BIOLOGICAL EVALUATION ; FACILE SYNTHESIS ; DERIVATIVES ; KINASE ; PROTOCOL
WOS研究方向	Chemistry
语种	英语
出版者	BENTHAM SCIENCE PUBL LTD
WOS记录号	WOS:000263979000007
内容类型	期刊论文
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.