Design and synthesis of an antitubercular compound,24-ketoarguesterol / 第三军医大学学报

ABSTRACT

Objective To design and synthesize an antitubercular compound,24-ketoarguesterol.Methods The target compound was synthesized via 8 steps,including methyl esterification,grignard isopropylation,deportation,etc.,using hyodeoxycholic acid as the starting material.3?-tert-butyldimethylsilyoxyl-5?-hydroxyl-6?-di-me-thoxylmethyl-24-keto-B-norcholanate was the key intermediate and grignard isopropylation as the key step.Results The target compound was synthesized in a total yield of 42% and identified by mass spectrometry(MS),proton magnetic resonance spectroscopy(1HNMR),carbon magnetic resonance spectroscopy,(13CNMR)and infrared spectroscopy(IR).Conclusion The synthetic route is characterized by atomic economy and high efficiency and laid the foundation for development of novel antituberculous drugs.