Synthesis method and application of cabardenafil analogue

• Main Authors: XIA JINTAO, JIANG FENG, ZHU SONGSONG, WU WANQIN
• Format: Patent
• Language: Chinese; English
• Published: 20.08.2024
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; METALLURGY; ORGANIC CHEMISTRY; PHYSICS; TESTING

The invention relates to the technical field of medicine, and provides a synthesis method and application of a cabardenafil analogue, the synthesis method comprises the following steps: firstly preparing 5-(2-ethoxyphenyl)-1-methyl-3-n-propyl-1, 6-dihydro-7H-pyrazolo [4, 3-d]-pyrimidine-7-ketone B, then preparing an intermediate C through a Friedel-Crafts acylation reaction, and finally preparing the cabardenafil analogue. And continuously carrying out alkaline oxidation-acidification reaction to prepare an intermediate D, and then carrying out acylation and amination reaction to obtain the phenylpropyl carbacdenafil. According to the synthesis method disclosed by the invention, the reaction steps and post-treatment are simplified, and further, by optimizing the substrate ratio, the reaction solvent, the temperature and the time of the Friedel-Crafts acylation reaction and the alkaline oxidation-acidification reaction, the yield of the phenylpropyl cabardenafil and the reproducibility of the reaction are grea