(S, S)-2, 8-diazabicyclo[4.3.0]nonane intermediate, and preparation method and application thereof

• Main Authors: FANG XIANG, DHILEEP KUMAR KRISHNAMURTHY, WANG JUN, HU RUIJUN, LU LIUCHUN, ZHAO LILAN, HU XINYING, GUO WENLONG, ZHANG YONGCHAI
• Format: Patent
• Language: Chinese; English
• Published: 11.06.2021
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a (S, S)-2, 8-diazabicyclo[4.3.0]nonane intermediate, and a preparation method and application thereof. New compounds, namely compounds II-V, are taken as key intermediates, a new route for synthesizing (S, S)-2, 8-diazabicyclo[4.3.0]nonane is developed, and in the route, dialkoxy acetate taken as an initial raw material in the route sequentially undergoes Claisen condensation, substitution reaction, intramolecular dehydration cyclization, catalytic hydrogenation reduction, chiral resolution, dissociation, hydrolysis, intramolecular dehydration cyclization and catalytic hydrogenation to obtain the(S, S)-2, 8-diazabicyclo[4.3.0]nonane. The preparation method is simple, the total reaction yield is high, the product quality is good, the process route is green and environment-friendly, and the method has a good industrial application prospect. 本发明公开了一种(S,S)-2,8-二氮杂双环[4.3.0]壬烷中间体及其制备方法和应用，本发明以新化合物-化合物II～V作为关键中间体，开发出一条新的合成(S,S)-2,8-二氮杂双环[4.3.0]壬烷的路线，该路线以二烷氧基乙酸酯作为起始原料，依次经过克莱森缩合、取代反应、分子内脱水环化、催