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First, when operating the DABCO-catalyzed Ireland-Claisen rearrangement of propargylic acrylates 18b-d, we added dienophiles 40a-f in the reaction system to capture the rearranged allenes products respectively. The Diels-Alder adducts 41a-i were obtained with complete regioselectivity. Thus a novel tandem Ireland-Claisen rearrangement /Diels-Alder reaction process with propargylic acrylates has been developed.

首先在进行DABCO-催化的丙烯酸炔丙酯类化合物18b-d的Ireland-Claisen重排反应的同时,于反应体系中分别加入亲二烯体40a-f捕获重排得到的连二烯中间体,一步反应获得了单一区域选择性的Diels-Alder环加成产物41a-i,从而创建了一条新颖的丙烯酸炔丙酯类化合物的Ireland-Claisen重排与Diels-Alder环加成的串联反应路线。

Improved synthesis of 2-(4-bromomethylphenyl)propionic acid,the key intermediate for loxoprofen sodium,was investigated.

对洛索洛芬钠的关键中间体2-(4-溴甲基苯基)丙酸的合成工艺进行了改进研究。

Aim To investigate a new synthetic method of 2-(4-bromomethylpheny1)propionic acid,the key intermediate of loxoprofen sodium.

摘要目的研究消炎镇痛药洛索洛芬钠的关键中间体2-4-溴甲基)苯基丙酸的合成新方法。

Results and conclusion The structure of 2-(4-bromomethylphenyl) propionic acid was identified by 1H-NMR, FT-IR and MS analysis. The target compound was prepared in an overall yield of 38%.

结果与结论关键中间体2-(4-溴甲基)苯基丙酸的结构经1H-NMR、FT-IR、MS谱确证,目标化合物的总收率为38%。

Results and conclusion The structure of 2-(4-bromomethylpheny1)propionic acid was identified by1H-NMR, FT-IR and MS analysis. The target compound was prepared in an overall yield of 38%.

结果与结论关键中间体2-4-溴甲基)苯基丙酸的结构经1H-NMR、FT-IR、MS谱确证,目标化合物的总收率为38%。

β-(3,5-Diterbutyl-4-hydroxyphenyl) propionyl chloride is synthesized with 3,5-methyl propionate as raw material via hydrolytic reaction and replacement reaction,and the replacement reaction conditions were explored.

摘 要:以β-(3,5-二叔丁基-4-羟基苯基)丙酸甲酯为原料,通过水解反应和酰氯合成反应合成了抗氧剂中间体β-(3,5-二叔丁基-4-羟基苯基)丙酰氯。

The introduction of cheap protonic acids can accelerate the formation of an active enanmine intermediate and stabilize the transition state by hydrogen bonding. Consequently, catalytic activity and enantioselectivity of the catalysis system are remarkably increased.

价廉易得的质子酸的引入不仅可促进活性中间体烯胺的生成,并可通过形成的氢键稳定反应的过渡态,从而显著提高该催化体系的催化活性和立体选择性。

The Research on Synthesis of 5-amino-3-cyan-N-(2, 6-dichloro-4-trifluoromethylphenyl) Pyrazole and Its Intermediates

中文名称: 5-氨基-3-氰基-N-(2,6-二氯-4-三氟甲基苯基)吡唑及其中间体的合成研究

Among them, pyrazole and its derivatives play an important part, exhibit better bioactivity and are becoming one kind of the most important leading structures in the fields of the organic synthesis.

在这些化合物中,吡唑类的化合物,尤其是吡唑类的芳环化合物被发现有着广泛的生物活性,因此成为了重要的药物研究先导结构,在很多有机合成及生物代谢过程中起着承上启下的中间体作用。

There was not few report about 5-amino-3-cyan-N-(2,6-dichloro-4-trifluoromethylphenyl)pyrazole in the domestic , so that the whole synthetic course of 5-amino-3-cyan-N-(2,6-dichloro-4-trifluoromethylphenyl)pyrazole was studied and the intermediate with feasible eco...

因此,研究5-氨基-3-氰基-N-(2,6-氯-4-三氟甲基苯基)吡唑的合成,探索其中间体经济可行的合成路线,具有很好的社会效益和经济前景。

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