3495-46-3Relevant articles and documents
Carbon Dioxide as a Directing Group for C-H Functionalization Reactions Involving Lewis Basic Amines, Alcohols, Thiols, and Phosphines for the Synthesis of Compounds
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Paragraph 0092; 0096; 0107, (2019/07/03)
Methods of synthesizing compounds using CO2 as a directing group for C—H functionalization, and compounds made thereby, are described.
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: Synthesis and in vitro, in vivo, and x-ray crystallographic characterization
Wright, Stephen W.,Ammirati, Mark J.,Andrews, Kim M.,Brodeur, Anne M.,Danley, Dennis E.,Doran, Shawn D.,Lillquist, Jay S.,McClure, Lester D.,McPherson, R. Kirk,Orena, Stephen J.,Parker, Janice C.,Polivkova, Jana,Qiu, Xiayang,Soeller, Walter C.,Soglia, Carolyn B.,Treadway, Judith L.,VanVolkenburg, Maria A.,Wang, Hong,Wilder, Donald C.,Olson, Thanh V.
, p. 3068 - 3076 (2007/10/03)
Inhibitors of the glucagon-like peptide-1 (GLP-1) degrading enzyme dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes in animal models and in human subjects. A novel series of cis-2,5-dicyanopyrrolidine α-amino amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes. 1-({[1-(Hydroxymethyl)cyclopentyl]amino}-acetyl)pyrrolidine-2,5-cis- dicarbonitrile (1c) is an achiral, slow-binding (time-dependent) inhibitor of DPP-IV that is selective for DPP-IV over other DPP isozymes and proline specific serine proteases, and which has oral bioavailability in preclinical species and in vivo efficacy in animal models. The mode of binding of the cis-2,5-dicyanopyrrolidine moiety was determined by X-ray crystallography. The hydrochloride salt of 1c was further profiled for development as a potential new treatment for type 2 diabetes.
Biologically selective potassium channel openers having 1,1- diethylpropyl group
Yoshiizumi, Kazuya,Seko, Norihiko,Nishimura, Noriyasu,Ikeda, Shoji,Yoshino, Kohichiro,Kondo, Hirosato,Tanizawa, Kazutaka
, p. 3397 - 3402 (2007/10/03)
To find out selective potassium channel openers (PCOs), we synthesized several 3,5-disubstituted phenylcyanoguanidine derivatives and investigated their structure-activity relationships (SAR). As a result, we discovered selective PCOs having 1,1-diethylpropyl group toward antihypertensive activity.