An economical and efficient approach to pharmaceutically and biologically significant 2,3dihydroquinazolin-4(1H)-ones has been disclosed. The one-pot multicomponent reaction was performed through a palladium-catalyzed ortho-selective oxidative carbonylation of N-substituted anilines with CO and primary amines, and subsequent condensation with aldehydes in MeCN by using alkylamino as the directing group, KI/AcOH as the additives, and Cu(OAc) 2 as the oxidant. This intriguing straightforward method features embedded directing strategy, simple starting materials, mild conditions, high atom/step economic economy, broad substrate scope and good product diversity.Keywords: CÀH activation; 2,3-dihydroquinazolin-4(1H)-ones; embedded directing group; N-alkyl anilines; palladium 2,3-Dihydroquinazolin-4(1H)-ones (DHQAs) are an important class of nitrogen-containing heterocycles with a wide range of pharmaceutical and biological activities such as anticancer, [1] 1 reverse transcriptase, [16] inosine 5'-monophosphate dehydrogenase, [17] protein kinase C-q, [18] transient receptor potential melastatin 2 19 inhibition. For exam-ple, evodiamine [2a,4a,20] and metolazone [10b,21] are typical representatives of clinically significant DHQA medications ( Figure 1).Due to their immense and important biological activities, the synthesis of DHQAs has attracted considerable interests. Among the established synthetic protocols, the typical procedures involve cyclocondensation of o-amino-benzamides (usually obtained by ammonolysis of isatoic anhydride) with aldehydes (Scheme 1a), [3a,22] reductive cyclization of onitrobenzamides or o-azidobenzamides with carbonyl compounds (Scheme 1b), [23] cyclocondensation of isatoic anhydrides, primary amines (or ammonium salts) and aldehydes (Scheme 1c), [2b,5a,22a,24] and cyclocondensation of o-aminobenzonitriles with carbonyl compounds (Scheme 1d). [25] Despite the above advances, however, one major drawback associated with all the above approaches is that the N 1 -containing starting materials applied in these protocols are usually Figure 1. Representative examples of clinically significant DHQA medications.