中文摘要：

以DDQ和TBN为催化剂,氧气为氧源,研究了罗素伐他汀母核合成过程中从多取代二氢嘧啶（I）转化为相应的嘧啶中间体（II）的氧化芳构化反应.考察了反应温度,反应溶剂及催化剂用量对氧化芳构化反应的影响.优化实验结果表明,以2%的DDQ及10%TBN为催化剂,氧气为氧源,在甲苯中60℃反应24 h,多取代二氢嘧啶完全转化,获得高选择性的氧化芳构化产物嘧啶中间体（II）.在50 mmol规模的氧化芳构化反应的实验中获得了98.8%的分离收率,反应的后处理方便简洁.

英文摘要：

A new catalytic system composed with DDQ/TBN for conversion of multi-substituted dihydro-pyrimidine（I） to Rosuvastatin pyrimidine intermediate via aerobic aromatization has been developed.The effects of reaction temperature,solvent and catalyst loading have been fully investigated on the aerobic oxidative aromatization.The optimal aerobic oxidation conditions for the quantitative conversion of multi-substituted dihydro-pyrimidine（I）,together with high selectivity of desired pyrimidine（II）,was obtained with 2% of DDQ,10% of TBN in toluene under 60 ℃ for 24 h.Up to 98.8% of isolated yield of the desired product was achieved in a 50 mmol scale through very simple work-up procedure.