- Michael addition reaction catalyzed by imidazolium chloride to protect amino groups and construct medium ring heterocycles
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An effective approach for amino protection and construction of a seven-membered ring has been developed. The method uses imidazolium chloride to carry out the Michael addition reaction at low temperatures and perform amino deprotection or construction of a seven-membered ring at high temperatures.
- Dai, Zeshu,Li, Dan,Li, Yanwu,Li, Zhiyao,Luo, Wen,Shang, Suqin,Tian, Qingqiang,Wang, Xuetong,Yuan, Jianyong,Zhang, Ying
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supporting information
(2019/12/04)
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- Method for catalyzing amino protection by imidazole hydrochloride
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The invention provides an amino protection method which realizes multi-substituted amino protection by using imidazole hydrochloric acid as an accelerator to push derivatives of primary amine, secondary amine and acrylamide to perform Michael addition at a relatively low temperature, wherein the imidazole hydrochloric acid promotes a carbon-nitrogen bond to crack back to the derivatives of primaryamine and acrylamide at a high temperature. The method provided by the invention is simple and economical, high in practicability, free of any other catalysts or additives, capable of protecting amino to have good functional group tolerance and excellent yield and purity, short in reaction time, free from harsh reaction conditions and suitable for industrial production.
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Paragraph 0039-0043
(2019/08/01)
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- Preparation method of 3-(phenyl amino)allylamines compound
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The invention belongs to the technical field of chemical synthesis, and particularly relates to a preparation method of a 3-(phenyl amino)allylamines compound. The method comprises the following stepsof mixing an aromatic amine compound and acrylamide, re
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Paragraph 0017; 0025; 0026; 0027; 0028; 0029; 0030
(2018/09/20)
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- Aza-Michael mono-addition using acidic alumina under solventless conditions
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Aza-Michael reactions between primary aliphatic and aromatic amines and various Michael acceptors have been performed under environmentally-friendly solventless conditions using acidic alumina as a heterogeneous catalyst to selectively obtain the corresponding mono-adducts in high yields. Ethyl acrylate was the main acceptor used, although others such as acrylonitrile, methyl acrylate and acrylamide were also utilized successfully. Bi-functional amines also gave the mono-adducts in good to excellent yields. Such compounds can serve as intermediates for the synthesis of anti-cancer and antibiotic drugs.
- Bosica, Giovanna,Abdilla, Roderick
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- Reductive N-alkylation of aromatic amines and nitro compounds with nitriles using polymethylhydrosiloxane
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The potential utility of polymethylhydrosiloxane (PMHS) as a reducing agent for reductive N-alkylation of aromatic amines and nitro compounds using nitriles as an alkylating agent and Pd(OH)2/C as a catalyst is described. The application of this method for the synthesis of several heterocyclic compounds is also reported.
- Reddy, Ch. Raji,Vijeender,Bhusan, P. Bibhuti,Madhavi, P. Phani,Chandrasekhar
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p. 2765 - 2768
(2008/02/03)
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