Patent classifications
C07J53/00
C17 POLAR-SUBSTITUTED HETEROAROMATIC SYNTHETIC TRITERPENOIDS AND METHODS OF USE THEREOF
Disclosed herein are compounds of the formula:
##STR00001##
wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used as antioxidant inflammation modulators. In some aspects, the present disclosure provides methods wherein the compounds and composition described herein are used for the treatment of diseases and disorders, including those associated with inflammation and cancer.
FULLY-CONTINUOUS SYNTHESIS METHOD OF CYPROTERONE ACETATE
A fully-continuous synthesis method of cyproterone acetate is provided. 4-androstene-3,17-dione is adopted as a starting material. The present disclosure adopts a fully continuous device composed of micromixers, microreactors, online gravity separation units, online solvent switching units, online solvent concentration units and solvent recovery systems connected according to a cyproterone acetate synthesis route. Cyproterone acetate product is synthesized through one enzymatic catalytic reaction, nine chemical reactions and continuous operations. This can realize recovery of dichloromethane, dichloroethane and ethanol, and significantly reduce emission of three wastes. The obtained crude cyproterone acetate is subjected to decolorization, recrystallization, filtration and drying to obtain pure cyproterone acetate with a purity greater than 99%.
Salt and crystal form of steroid derivative regulator
The present invention relates to a steroid derivative regulator, in particular to a compound of formula (I), a salt and crystal form thereof, a preparation method therefor, a pharmaceutical composition containing a therapeutically effective amount of the crystal form, and an application thereof as a GABA.sub.A receptor regulator in treatment of depression, convulsions, Parkinsonism and nervous system diseases. ##STR00001##
Process for the preparation of drospirenone as a fine powder through a double change of crystalline form
The present invention refers to a process for the industrial-scale preparation of 17-hydroxy-6,7; 15,16-dimethylene-3-oxo-17-pregn-4-ene-21-carboxylic acid -lactone, known by the common name of Drospirenone, in the form of a fine powder without the use of mechanical grinding or micronization techniques, but rather exploiting a double change of crystalline form, from Crystalline Form I to Crystalline Form II and from Crystalline Form II to Crystalline Form I. The invention also refers to the new Crystalline Form II of Drospirenone obtained in the process.