Synthesis of Novel Thiazolo[3,2-a]pyrimidine Compounds

5-乙氧羰基-4-芳基-6-甲基-3,4-二氢嘧啶-2-酮与丁炔二酸二甲酯反应,合成了系列新的噻唑并[3,2-A]嘧啶类化合物,反应具有时间短、收率高、后处理简单等优点.采用nMr(1H,13C,COSy,HSQC和HMbC),Ir等多种谱学技术,结合元素分析对产物进行详细表征,通过对目标产物的1,3-偶极环加成的衍生化产物进行X射线单晶衍射而确定目标产物的结构.A new class of thiazolo[3,2-a]pyrimidine compounds were synthesized by the reaction of 5-carbethoxyl-4-aryl-6-methyl-1,2,3,4-tetrahydropyrimidin-2-ones with dimethyl acetylenedicarboxylate.The reaction has the advantages of excellent yields and simple workup procedures.The products were char-acterized thoroughly by IR and NMR(1H,13C,COSY,HSQC and HMBC) together with elemental analysis.The X-ray crystallographic analysis of the 1,3-dipolar cycloaddition derivative of the title product provided the direct information for the structure of the product.国家自然科学基金(Nos.20772027;20803020);中国博士后科学基金(No.20070410805);卫生部科学研究基金-福建省卫生教育联合攻关计划(No.WKJ2008-2-036);厦门市重大疾病攻关研究基金(No.3502Z20051027);湖南科技大学博士基金(No.E50839)资助项

Synthesis of Novel Thiazolo[3,2-a]pyrimidine Compounds

A new class of thiazolo[3,2-a]pyrimidine compounds were synthesized by the reaction of 5-carbethoxyl-4-aryl-6-methyl-1,2,3,4-tetrahydropyrimidin-2-ones with dimethyl acetylenedicarboxylate. The reaction has the advantages of excellent yields and simple workup procedures. The products were characterized thoroughly by IR and NMR (H-1, C-13, COSY, HSQC and HMBC) together with elemental analysis. The X-ray crystallographic analysis of the 1,3-dipolar cycloaddition derivative of the title product provided the direct information for the structure of the product