22042-72-4Relevant articles and documents
Preparation method of silodosin intermediate
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Paragraph 0043-0046; 0053-0056; 0063-0066; 0073-0076, (2019/04/13)
The invention discloses a preparation method of a silodosin intermediate and relates to the technical field of chemical synthesis of drugs. The preparation method comprises the following steps: subjecting salicyaldehyde and ethylene carbonate to transesterification to obtain 2-(2-hydroxyethoxy)benzaldehyde; then, carrying out a Dakin oxidation reaction to obtain sodium 2-(2-hydroxyethoxy) phenol;then, subjecting sodium 2-(2-hydroxyethoxy) phenol and trifluoroethanol to an etherification reaction to obtain 2-[2-(2,2,2-trifluoroethyoxy)phenoxy]ethyl alcohol; and finally, subjecting 2-[2-(2,2,2-trifluoroethyoxy)phenoxy]ethyl alcohol and methanesulfonyl chloride to an esterfication reaction to obtain the silodosin intermediate 2-[2-(2,2,2-trifluoroethyoxy)phenoxy]ethyl methanesulfonate. The preparation method is novel and short in synthesis route, and a target product can be prepared by only four-step reaction. Both raw materials and reagents used for preparation are cheap, available andenvironment-friendly, all the reaction conditions are mild and controllable, the preparation method is convenient and simple in operation, and the prepared silodosin intermediate is high in purity andyield, suitable for industrial production and wide in prospect and industrial application value.
N-heterocyclic carbene catalyzed nucleophilic substitution reaction for construction of benzopyrones and benzofuranones
He, Jinmei,Zheng, Jiyue,Liu, Jian,She, Xuegong,Pan, Xinfu
, p. 4637 - 4640 (2007/10/03)
N-Heterocyclic carbene as an efficient organic catalyst was employed to catalyze an intramolecular nucleophilic substitution reaction. When R 2 was a phenyl group, the cyclization process underwent isomerization, leading to generation of benzofuranone.
1,4-dihydropyridine derivatives
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, (2008/06/13)
Compounds a formula (I) STR1 wherein the substituents and symbols have the meanings given in the specification, are new compounds with marked cardiovascular activity.