Author(s): Chunhao Yang, Haofei Yu, Na Yang, Linghua Meng, Jing Xu, Rongping Zhang, Yuyuan Xie and Jian Ding
Page: [134 - 140] Pages: 7
* (Excluding Mailing and Handling)
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.
Keywords: Baylis-Hillman adducts, PI3K inhibitors, pyrimidin-4(3H)-one, dihydropyrimidin-4(3H)-one
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