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新型绿色室温离子液体催化合成monastrol及其衍生物
袁文琳¹,夏天一¹,沈颂章²,王小燕²,何邦平²,孙青^3*
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(1. 第二军医大学研究生管理大队药学队，上海 200433 2. 第二军医大学药学院实验教学中心，上海 200433 3. 第二军医大学药学院有机化学教研室，上海 200433 ^*通信作者)

摘要:

目的探索操作简便的monastrol及其衍生物的绿色合成方法。方法以(取代)苯甲醛、乙酰乙酸乙酯和硫脲(或尿素)作为起始原料，在微波加热、无溶剂条件下，采用自行设计的绿色室温离子液体1-丁基-3-甲基咪唑-L-樟脑磺酸盐催化Biginelli反应合成monastrol及其衍生物。结果该离子液体在微波加热、无溶剂条件下可催化Biginelli反应合成monastrol及其衍生物，且操作过程简单、反应时间短、环境友好。结论以新型绿色室温离子液体1-丁基-3-甲基咪唑-L-樟脑磺酸盐作为催化剂，经微波、无溶剂Biginelli反应合成monastrol及其衍生物是一种方法简单、操作方便、反应温和的绿色合成方法。

关键词: 室温离子液体 monastrol Biginelli反应 1-丁基-3-甲基咪唑-L-樟脑磺酸盐微波

DOI：10.3724/SP.J.1008.2011.01019

投稿时间：2011-05-29修订日期：2011-06-23

基金项目:第二军医大学大学生创新能力培养研究课题 (MS2010043, ZD2009001).

A new green room temperature ionic liquid catalyzes synthesis of monastrol and its derivatives through Biginelli reaction

YUAN Wen-lin¹,XIA Tian-yi¹,SHEN Song-zhang²,WANG Xiao-yan²,HE Bang-ping²,SUN Qing-yan^3*

(1. Pharmacy Team, School of Graduate Students, Second Military Medical University, Shanghai 200433, China
2. Center for Laboratory Teaching, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
3. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
^*Corresponding author.)

Abstract:

ObjectiveTo explore an easily-controllable, environmentally-friendly method for synthesizing monastrol and its derivatives. MethodsMonastrol and its derivatives were synthesized using (substituted) benzaldehyde, ethyl acetoacetate and thiourea (or urea) as the material through a Biginelli reaction catalyzed by green room temperature ionic liquid 1-butyl-3-methylimidazolium-L-camphorsulfonate under microwave irradiation without solvent. ResultsThe green room temperature ionic liquid 1-butyl-3-methylimidazolium-L-camphorsulfonate catalyzed Biginelli reaction in obtaining the title compound under microwave irradiation without solvent. The process was easy to operate, time saving and environmentally-friendly. ConclusionMicrowave-accelerated solvent-free Biginelli reaction using green room temperature ionic liquid 1-butyl-3-methylimidazolium-L-camphorsulfonate as catalyst is a convenient and environmentally-friendly method for synthesizing monastrol and its derivatives.

Key words: room temperature ionic liquids monastrol Biginelli reaction 1-butyl-3-methylimidazolium-L-camphorsulfonate microwaves