2,3-Dihydroquinazolin-4(1H)-one compounds are an important class of nitrogen-containing fused heterocycles, which possess a wide range of pharmacological and biological activities and have important applications in the fields of synthesis and research & development of drugs. Therefore, its synthetic methods have also attracted considerable attention. In this paper, the main advances in the synthesis of 2,3-dihydroquinazolin-4(1H)-ones and their proposed reaction mechanisms from the raw materials such as o-aminobenzamides, isatoic anhydrides, o-nitrobenzamides, o-azidobenzamide, o-bromobenzamide, o-bromobenzonitrile, o-aminobenzoic acids, o-aminobenzonitrile, o-amino-N-(propa-1,2-dienyl)benzamides, and N-alkyl anilines were introduced and reviewed, respectively. Finally, the synthesis of these compounds was summarized and the prospect of their development was prospected. Keywords 2,3-dihydroquinazolin-4(1H)-one; o-aminobenzamides; isatoic anhydrides; N-alkyl anilines; C-H activation & functionalization; palladium catalysis 2,3-二氢喹唑啉-4(1H)-酮是一类重要的含氮稠杂环 化合物, 具有抗癌 [1～3] 、抗肿瘤 [4～6] 、治疗高血压 [7～9] 、 抗炎 [10～12] 、抗菌 [13～15] 、利尿 [9,16,17] 、抗病毒 [18] 、抗痉 挛 [19] 、抑制疟原虫增殖 [20] 、驱虫 [21] 、镇痛 [12] 等作用以 及抑制组织蛋白酶 B&H [22] 、胆碱酯酶 [23,24] 、凝血因子 Xa [25] 、肌苷 5'-一磷酸脱氢酶 [26] 、蛋白激酶 C-θ [27] 、瞬 时受体电位通道 M2 [28] 等广泛的药理及生物活性; 此外, 该类化合物也很容易被氧化成其喹唑啉-4(3H)-酮类似 物, 后者通常作为重要模块用于构建天然产物 [29～31] 及 药物分子 [32～34]. 由于 2,3-二氢喹啉-4(1H)-酮类化合物具有广泛且重 要的生物活性及应用价值, 其合成方法也自然引起了人 们的极大兴趣和关注.根据国内外的研究动态, 对其主 要合成方法进行了总结.