373608-50-5Relevant articles and documents
CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
-
Page/Page column 172; 198, (2021/11/26)
This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
Preparation method of Volasertib intermediate 1-cyclopropyl methyl piperazine
-
Paragraph 0029; 0034, (2018/09/08)
The invention provides a preparation method of a Volasertib intermediate 1-cyclopropyl methyl piperazine. The preparation method comprises the following steps: S1, adding N-Boc-piperazine into an inert solvent and triethylamine or pyridine, dropwise adding cyclopropanecarbonyl chloride, adding water for extraction after the reaction ends, obtaining an organic phase, and concentrating the organic phase to remove an organic solvent to obtain a solid; S2, adding the solid obtained in S1 into an ether solvent, then adding sodium borohydride, dropwise adding boron trifluoride-diethyl ether for reaction, quenching the mixture, then extracting the mixture, and concentrating the mixture to remove an organic solvent to obtain a solid; S3, adding the solid obtained in S2 into an alcohol solvent, dropwise adding concentrated hydrochloric acid for reaction, alkalizing the mixture with sodium hydroxide or potassium hydroxide aqueous solution, and performing extraction and concentration in sequenceto obtain the compound 1-cyclopropyl methyl piperazine. The raw materials used in the preparation method are readily available, and the preparation method is low in cost, easy to operate, high in safety, high in product quality and yield, and convenient for large-scale production.
POLY (ADP-RIBOSE) POLYMERASE INHIBITOR
-
Paragraph 0115; 0116, (2015/02/25)
Disclosed are a phthalic hydrazide (phthalazine ketone) compound, and a pharmaceutical composition comprising the same. As a DNA repair enzyme poly (ADP-ribozyme) polymerase inhibitor, the compound and the pharmaceutical composition can effectively treat diseases involving PARP enzymatic activity, including cancer, neural degenerative diseases, inflammation and the like.