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Li, Bryan; Samp, Lacey; Sagal, John; Hayward, Cheryl M; Yang, Christine; Zhang, Zhijun
Journal of organic chemistry, 02/2013, Letnik: 78, Številka: 3Journal Article
Pyrido4,3-dpyrimidin-4(3H)-one (1) was prepared by reacting 2-trifluoromethyl-4-iodo-nicotinic acid (2) with amidine 9a catalyzed by Pd2(dba)3 and Xantphos, followed by cyclization effected with HBTU and subsequent demethylation using PhBCl2. The amidine arylation method was found applicable for the syntheses of quinazolin-4(3H)-ones. Thus, reaction of 2-bromo or 2-iodo benzoate esters with amdidines afforded substituted quinazolin-4(3H)-ones in 44–89% yields.
