Abstract: Disclosed is a one-pot process for the preparation of a prednisolone derivative of formula I, comprising reacting the compound of formula II with the compound of formula III and the compound of formula IV The process does not need to separate and purify the intermediate formed, and therefore the process reduces the reaction time and increases the yield of the product compared to the prior art.
Abstract: The present invention relates to oripavine derivatives of formula (I), wherein R1 is hydrogen or methyl, R2 is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R3 is thiophenyl ethyl or cycloalkyl methyl where the cycloalkyl has 3 to 6 carbon atoms, or non-toxic pharmaceutically acceptable salts thereof. These compounds can be used for the preparation of analgesics or abstinence agents of opium habit-forming drugs.
Type:
Grant
Filed:
September 13, 2002
Date of Patent:
October 10, 2006
Assignees:
Institute of Pharmacology and Toxicology Academy of Military Medical Sciences, P.L.A. China, Zhejiang Xianju Pharmaceuticals Co. Ltd.
Inventors:
Bohua Zhong, Zehui Gong, Yaping Wang, Yongshao Liu
Abstract: The present invention concerns with steroid compounds of formula (I)
wherein R1 is cyclohexyl or cycloheptyl, R2 is hydrogen or C1-C6 alkyl, R3 is hydrogen, C1-C6 alkyl or methylol, R4 is hydrogen or hydroxymethylene and a pharmaceutically acceptable salt thereof. The invention also concerns with a method for preparation of the compounds, pharmaceutical compositions containing the compounds as its active component and use of the compounds and the pharmaceutical compositions in preparing medicines for treating diseases, e.g. those associated with progestin dependence.