1228780-72-0Relevant articles and documents
Mild and Robust Stille Reactions in Water using Parts Per Million Levels of a Triphenylphosphine-Based Palladacycle
Takale, Balaram S.,Thakore, Ruchita R.,Casotti, Gianluca,Li, Xaiohan,Gallou, Fabrice,Lipshutz, Bruce H.
, p. 4158 - 4163 (2021/02/01)
An inexpensive and new triphenylphosphine-based palladacycle has been developed as a pre-catalyst, leading to highly effective Stille cross-coupling reactions in water under mild reaction conditions. Only 500–1000 ppm of Pd suffices for couplings involving a variety of aryl/heteroaryl halides with aryl/hetaryl stannanes. Several drug intermediates can be prepared using this catalyst in aqueous nanoreactors formed by 2 wt % Brij-30 in water.
Venetoclax and dihydroartemisinin compound and preparation method and application thereof
-
, (2021/03/05)
The invention belongs to the technical field of medicines, and relates to a Venetoclax and dihydroartemisinin compound, pharmaceutically acceptable salts, hydrates and optical isomers thereof, a pharmaceutical composition taking the compound as an active component, and an application of the compound in preparation of medicines for treating cancers. The structure of the Venetoclax and dihydroartemisinin compound is as shown in a general formula I in the specification, wherein L is as described in the claims and the specification.
Solid dispersions containing an apoptosis-inducing agent
-
, (2019/03/15)
A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.