Identification of selective inhibitors of cyclin dependent kinase 4
作者:David J Carini、Robert F Kaltenbach、Jie Liu、Pamela A Benfield、John Boylan、Michael Boisclair、Leonardo Brizuela、Catherine R Burton、Sarah Cox、Robert Grafstrom、Barbara A Harrison、Kimberly Harrison、Emeka Akamike、Jay A Markwalder、Yuki Nakano、Steven P Seitz、Diane M Sharp、George L Trainor、Thais M Sielecki
DOI:10.1016/s0960-894x(01)00416-4
日期:2001.8
A new structural type of kinase inhibitor, containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the cyclindependentkinase family of enzymes. Although the cdks are highly homologous, representatives of the series showed intra-cdk selectivities, especially for cdk4. SAR studies elucidated the important features of the molecules for inhibition
The first example of Pd-catalyzed Suzukicross-coupling of readily available arylhydrazines with arylboronic acids via C–N bond cleavage was developed under air, affording various biaryl compounds with broad substrate applicability and moderate to good yields. Moreover, the rigorous exclusion of air/moisture is not required in these transformations. Thus, the protocol represents a simple and efficient
One-Pot Synthesis of Indoles and Pyrazoles via Pd-Catalyzed Couplings/Cyclizations Enabled by Aqueous Micellar Catalysis
作者:Evan B. Landstrom、Nnamdi Akporji、Nicholas R. Lee、Christopher M. Gabriel、Felipe C. Braga、Bruce H. Lipshutz
DOI:10.1021/acs.orglett.0c02315
日期:2020.8.21
aminations followed by subsequent cyclizations facilitated by aqueous micellar catalysis. This new technology includes efficient couplings with low loadings of palladium, a more stable source of the required hydrazine moiety, greater atom economy for the initial coupling, and reduced reaction temperatures, all leading to environmentally responsible processes.
Mild and Rapid Pd-Catalyzed Cross-Coupling with Hydrazine in Continuous Flow: Application to the Synthesis of Functionalized Heterocycles
作者:Andrew DeAngelis、Dong-Hui Wang、Stephen L. Buchwald
DOI:10.1002/anie.201208544
日期:2013.3.18
CN cross‐coupling of aryl chlorides with hydrazine is described. Through the use of continuousflow, the hazards associated with the use of hydrazine in the presence of transition metals are decreased. In addition, multistep flow sequences have also been developed for the generation of functionalizedheterocycles utilizing the arylhydrazine intermediates.