885126-34-1Relevant articles and documents
Safe, Scalable, Inexpensive, and Mild Nickel-Catalyzed Migita-Like C?S Cross-Couplings in Recyclable Water
Yu, Tzu-Yu,Pang, Haobo,Cao, Yilin,Gallou, Fabrice,Lipshutz, Bruce H.
, p. 3708 - 3713 (2020/12/17)
A new approach to C?S couplings is reported that relies on nickel catalysis under mild conditions, enabled by micellar catalysis in recyclable water as the reaction medium. The protocol tolerates a wide range of heteroaromatic halides and thiols, including alkyl and heteroaryl thiols, leading to a variety of thioethers in good isolated yields. The method is scalable, results in low residual metal in the products, and is applicable to syntheses of targets in the pharmaceutical area. The procedure also features an associated low E Factor, suggesting a far more attractive entry than is otherwise currently available, especially those based on unsustainable loadings of Pd catalysts.
ALKYNYL INDAZOLE DERIVATIVE AND USE THEREOF
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, (2017/02/24)
The main object of the present invention is to provide a novel compound which has a VEGF receptor tyrosine kinase inhibitory activity and is useful as an active ingredient for the treatment of diseases accompanying angiogenesis or edema, for example, age-related macular degeneration or the like. The present invention includes, for example, an alkynyl indazole derivative represented by the following general formula (I), a pharmaceutical acceptable salt thereof, and a medicine containing thereof.
Development of an efficient Pd-catalyzed coupling process for axitinib
Chekal, Brian P.,Guinness, Steven M.,Lillie, Brett M.,McLaughlin, Robert W.,Palmer, Charles W.,Post, Ronald J.,Sieser, Janice E.,Singer, Robert A.,Sluggett, Gregory W.,Vaidyanathan, Rajappa,Withbroe, Gregory J.
, p. 266 - 274 (2014/05/20)
The manufacturing process of axitinib (1) involves two Pd-catalyzed coupling reactions, a Migita coupling and a Heck reaction. Optimization of both of these pivotal bond-formation steps is discussed as well as the approach to control impurities in axitinib. Essential to the control strategy was the optimization of the Heck reaction to minimize formation of impurities, in addition to the development of an efficient isolation of crude axitinib to purge impurities.
