Abstract A reproducible and scalable method has been developed for the synthesis of a series 3,6-substituted pyrazolo[1,5- ]pyrimidines, which are basis rational design selective inhibitors AMP-activated protein kinase. Regarding formation new types carbon skeleton, applicability Suzuki–Miyaura cross-coupling using Buchwald ligands to form C–C bond in sterically hindered position 6 5,7-dimethyl...

Unusual 2,7-diazacarbazoles were prepared in one step from readily available tetra-halogenated 4,4'-bipyridines by using a double N-arylation reaction in the presence of the Pd-XPhos catalyst system. Moderate to good yields were obtained in this site-selective Buchwald-Hartwig double amination. The functionalization of these tricyclic derivatives was performed by using Pd-catalyzed cross-coupli...

Inspired by naturally occurring molecules containing atropisomeric N+-C axes, we have developed a novel synthetic approach to generate library of axially chiral N-aryl quinolinium salts. Enantiopurities up 93 % ee were obtained via four-step route from commercially available precursors. Axial stereochemistry was controlled through an enantioselective ring-closing Buchwald–Hartwig coupling react...

A novel two step protocol was developed to gain regiospecific access to 3-substituted β- and aza-β-carbolines, 3-PBC (1), 3-ISOPBC (2), βCCt (3), 6-aza-3-PBC (4) and 6-aza-3-ISOPBC (5). These β-carbolines (1-3) are potential clinical agents to reduce alcohol self-administration, especially 3-ISOPBC·HCl (2·HCl) which appears to be a potent anti-alcohol agent active against binge drinking in a ra...

1,2J T KOWALLICK, 2,3A A JOSEPH, PhD, 2,4C UNTERBERG-BUCHWALD, MD, 1,2M FASSHAUER, MD, 5K VAN WIJK, PhD, 3K D MERBOLDT, PhD, 3D VOIT, PhD, 2,3J FRAHM, PhD,1,2J LOTZ, MD and 1,2J M SOHNS, MD Institute for Diagnostic and Interventional Radiology, Heart Center, University Medical Center Göttingen, Göttingen, Germany DZHK, German Center for Cardiovascular Research, partnersite Göttingen, Göttingen,...

A survey of carotenoid—protein complexes is presented. Distinction is made between astaxanthin—proteins in which the absorption band of the carotenoid is unaltered in shape, and carotenoid—lipoglycoprotein complexes. The proposal by Buchwald and Jencks79 that the carotenoid is twisted about the double bonds of the polyene chain, is discussed and sustained for astaxanthin—proteins. A mode of bin...

Front Cover: In article number 2000520 by Myungeun Seo, Wonhee Lee, and co-workers, a cross-coupling reaction is utilized for polymer surface modification. Poly(chloro-p-xylylene) (parylene C) used as substrate in Pd-catalyzed Buchwald–Hartwig amination to install primary amine groups. Parylene films with microscale topography can be successfully modified chemically bonded fabricate transparent...