19869-42-2Relevant articles and documents
Method for preparing N-methyl azepine-4-one hydrochloride
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, (2021/06/09)
The invention discloses a method for preparing N-methyl azepine-4-one hydrochloride. According to the method, 4-oxime cyclohexanone is taken as a raw material, aza-cycloheptane-2,5-diketone is obtained under a Beckmann rearrangement condition, aza-cycloheptane-2,5-diketone and ethylene glycol are subjected to condensation to generate ketal, amide is reduced through red aluminum, methylation is performed, ethylene glycol is removed under a hydrochloric acid condition, and finally N-methyl azepine-4-one hydrochloride is obtained. The invention provides a safe, reliable and efficient synthetic route, the raw materials are low in price, the reaction conditions are mild, explosive diazomethane does not need to be used, methyl acrylate which is easy to polymerize and high in carcinogenesis is also not needed, and the method is more suitable for large-scale industrial production.
Method for the preparation of hexahydroazepinones and hexahydroazepinoles
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, (2008/06/13)
This disclosure describes two technical procedures for the high-yield synthesis of heterocyclic seven-membered ring-systems by Dieckmann-condensation avoiding usual dilution techniques and long reaction times. Thus, it significantly increases the overall yields of the pharmaceutically active ingredients azelastine and flezelastine, whose synthesis, starting from these seven-membered heterocyclic rings, is reported elsewhere. Yields range from 80-89%, avoiding waste and increasing economics of the synthesis.