2985-50-4Relevant articles and documents
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors
Yamashita, Dennis S.,Marquis, Robert W.,Xie, Ren,Nidamarthy, Sirishkumar D.,Oh, Hye-Ja,Jeong, Jae U.,Erhard, Karl F.,Ward, Keith W.,Roethke, Theresa J.,Smith, Brian R.,Cheng,Geng, Xiaoliu,Lin, Fan,Offen, Priscilla H.,Wang, Bing,Nevins, Neysa,Head, Martha S.,Haltiwanger, R. Curtis,Sarjeant, Amy A. Narducci,Liable-Sands, Louise M.,Zhao, Baoguang,Smith, Ward W.,Janson, Cheryl A.,Gao, Enoch,Tomaszek, Thaddeus,McQueney, Michael,James, Ian E.,Gress, Catherine J.,Zembryki, Denise L.,Lark, Michael W.,Veber, Daniel F.
, p. 1597 - 1612 (2006)
The syntheses, in vitro characterizations, and rat and monkey in vivo pharmacokinetic profiles of a series of 5-, 6-, and 7-methyl-substituted azepanone-based cathepsin K inhibitors are described. Depending on the particular regiochemical substitution and
Base-catalysed intramolecular hydroamination of vinyl sulfiies
Quinet, Coralie,Sampoux, Laetitia,Marko, Istvan E.
supporting information; experimental part, p. 1806 - 1811 (2009/09/06)
Small amounts of n-butyllithium catalyse the highly efficient hydroamination of a large variety of vinyl sulfides. This novel methodology offers an easy access to a wide range of nitrogen heterocycles, including simple pyrrolidines and piperidines, as well as more complex bicyclic compounds. Subsequent transformations of the sulfur group led to the formation of functionalised alkaloid-like substructures. Wiley-VCH Verlag GmbH & Co. KGaA.
P(RNCH2CH2)3N: Efficient 1,4-addition catalysts
Kisanga, Philip B.,Ilankumaran, Palanichamy,Fetterly, Brandon M.,Verkade, John G.
, p. 3555 - 3560 (2007/10/03)
The 1,4-addition of primary alcohols, higher nitroalkanes, and a Schiff's base of an α-amino ester to α,β-unsaturated substrates produces the corresponding products in moderate to excellent yields when carried out at -63 to 70°C in the presence of catalytic amounts of the nonionic strong bases P(RNCH2CH2)3N (R = Me, i-Pr, i-Bu) in isobutyronitrile. Diastereoselectivity for the anti form of the product is high in the case of the Schiff's base in the absence of lithium ion. These catalysts are easily removed from the product by either column filtration through silica gel or via aqueous workup.
