Inorganic drug technology innovation process

Synthetic rebamipide

Xu Xiufeng and other scientific and technological personnel of the New Laboratory of Reactors and Green Chemical Processes of Wuhan University of Engineering have repeatedly studied and proposed a new process for the synthesis of rebamipide: using diethyl malonate as the starting material, nitrosation reaction And reduction reaction to prepare diethylaminomalonate; and then 4-bromomethylquinolin-2-one by condensation reaction to obtain 2-(4-aminobenzamide)-3-(1,2- Dihydro-2-oxo-4-quinolinyl)malonic acid diethyl ester; then the anti-ulcer drug rebamipide was obtained by hydrolysis and decarboxylation under base catalysis, and the total yield was about 71.7%. The raw material of the process is relatively cheap, the synthesis steps are less, and the reaction yield of each step is higher.

Synthetic rufinamide

Science and technology personnel such as Ju Wenjian from the Department of Medicinal Chemistry, China Pharmaceutical University proposed a new process for the synthesis of rufinamide: 2,6-difluorotoluene was used as the starting material, and 2,6-difluorobromide was obtained by bromination reaction with NBS. Benzyl, and then reacted with sodium azide to obtain 2,6-difluorobenzyl azide, which is then cyclized with methyl propiolate to give 1-[(2,6-difluorophenyl)methyl]-1H. -1,2,3-triazole-4-carboxylic acid methyl ester, after the Zui, the anti-epileptic drug Lufinamide was obtained by aminolysis reaction, and the total reaction yield was about 47%.

Synthetic palonosetron

Du Youguo and other scientific and technical personnel of Jiangsu Osei Kang Pharmaceutical Co., Ltd. have repeatedly studied and proposed a new process for the synthesis of palonosetron: (S)-1,2,3,4-tetrahydro-1-naphthoic acid As a starting material, after multiple steps of acylation, condensation, reduction, cyclization, salt formation, etc., palinosetron hydrochloride is finally synthesized, and the total reaction yield is about 36.2%. The reaction operation of each step of the synthetic route is relatively simple, does not require a special reaction device, is less difficult to synthesize, and is easy to industrialize.


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