199679-74-8Relevant articles and documents
Enantioselective Synthesis of Chiral Carboxylic Acids from Alkynes and Formic Acid by Nickel-Catalyzed Cascade Reactions: Facile Synthesis of Profens
Fu, Kaiyue,Ma, Yu,Sun, Yaxin,Tang, Bo,Yang, Guang,Yang, Peng,Yue, Jieyu,Zhang, Li,Zhou, Jianrong Steve
supporting information, (2021/11/22)
We report a stereoselective conversion of terminal alkynes to α-chiral carboxylic acids using a nickel-catalyzed domino hydrocarboxylation-transfer hydrogenation reaction. A simple nickel/BenzP* catalyst displayed high activity in both steps of regioselective hydrocarboxylation of alkynes and subsequent asymmetric transfer hydrogenation. The reaction was successfully applied in enantioselective preparation of three nonsteroidal anti-inflammatory profens (>90 % ees) and the chiral fragment of AZD2716.
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor
Tran, Joe A.,Jiang, Wanlong,Tucci, Fabio C.,Fleck, Beth A.,Wen, Jenny,Sai, Yang,Madan, Ajay,Ta, Kung Chen,Markison, Stacy,Foster, Alan C.,Hoare, Sam R.,Marks, Daniel,Harman, John,Chen, Caroline W.,Arellano, Melissa,Marinkovic, Dragan,Bozigian, Haig,Saunders, John,Chen, Chen
, p. 6356 - 6366 (2008/03/30)
Benzylamine and pyridinemethylamine derivatives were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC4R). These compounds were also profiled in rodents for their pharmacokinetic properties. Two compounds with diversified profiles in chemical structure, pharmacological activities, and pharmacokinetics, 10 and 12b, showed efficacy in an established murine cachexia model. For example, 12b had a Ki value of 3.4 nM at MC4R, was more than 200-fold selective over MC3R, and had a good pharmacokinetic profile in mice, including high brain penetration. Moreover, 12b was able to stimulate food intake in the tumor-bearing mice and reverse their lean body mass loss. Our results provided further evidence that a potent and selective MC4R antagonist with appropriate pharmacokinetic properties might potentially be useful for the treatment of cancer cachexia.
Highly rigid diphosphane ligands with a large dihedral angle based on a chiral spirobifluorene backbone
Cheng, Xu,Zhang, Qi,Xie, Jian-Hua,Wang, Li-Xin,Zhou, Qi-Lin
, p. 1118 - 1121 (2007/10/03)
High and wide: The high rigidity and large dihedral angle of chiral, spirobifluorene-based diphosphane ligands lead to excellent reactivity and enantioselectivity in the ruthenium-catalyzed asymmetric hydrogenation of α,β-unsaturated carboxylic acids (see scheme).
