碘催化下二氢嘧啶在室温的多组分合成及其体外抗分枝杆菌活性
Multi-component synthesis of dihydropyrimidines by iodine catalyst at ambient temperature and in-vitro antimycobacterial activity.
作者信息
Zalavadiya Paresh, Tala Satish, Akbari Jignesh, Joshi Hitendra
机构信息
Chemical Research Laboratory, Department of Chemistry, Saurashtra University, Rajkot Gujarat, India.
出版信息
Arch Pharm (Weinheim). 2009 Aug;342(8):469-75. doi: 10.1002/ardp.200800224.
An efficient and simple three-component domino synthesis of some new dihydropyrimidines (DHPMs) from aromatic aldehydes, 1,3-dicarbonyl compounds and N-(3-chloro-4-fluorophenyl)urea using molecular iodine as catalyst is described. The 1-substituted dihydropyrimidines were isolated in good to excellent yields (78-90%) within a short reaction time (4-6 h) at ambient temperature. The biological evaluation revealed that the newly synthesized compounds (4a-i and 5a-i) exhibited moderate antimycobacterial activity against Mycobacterium tuberculosis H(37) RV.
描述了一种高效且简单的由芳香醛、1,3 - 二羰基化合物和N - (3 - 氯 - 4 - 氟苯基)脲通过分子碘催化的三组分多米诺合成法来合成一些新型二氢嘧啶（DHPMs）。在环境温度下，1 - 取代二氢嘧啶在短反应时间（4 - 6小时）内以良好至优异的产率（78 - 90%）被分离出来。生物学评估表明，新合成的化合物（4a - i和5a - i）对结核分枝杆菌H(37) RV表现出适度的抗分枝杆菌活性。
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