Synthesis of Quinazolin-4 (3 H)-ones via Amidine N-Arylation

…, L Samp, J Sagal, CM Hayward, C Yang…

文献索引：Li, Bryan; Samp, Lacey; Sagal, John; Hayward, Cheryl M.; Yang, Christine; Zhang, Zhijun Journal of Organic Chemistry, 2013 , vol. 78, # 3 p. 1273 - 1277

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被引用次数: 26

摘要

Pyrido [4, 3-d] pyrimidin-4 (3 H)-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 (3 H)-ones. Thus, reaction of 2-bromo or 2-iodo benzoate esters with amdidines afforded substituted ...