92906-86-0Relevant academic research and scientific papers
Iridium-Catalyzed Highly Enantioselective Transfer Hydrogenation of Aryl N-Heteroaryl Ketones with N-Oxide as a Removable ortho-Substituent
Liu, Qixing,Wang, Chunqin,Zhou, Haifeng,Wang, Baigui,Lv, Jinliang,Cao, Lu,Fu, Yigang
supporting information, p. 971 - 974 (2018/02/23)
A highly enantioselective transfer hydrogenation of non-ortho-substituted aryl N-heteroaryl ketones, using readily available chiral diamine-derived iridium complex (S,S)-1f as a catalyst and sodium formate as a hydrogen source in a mixture of H2O/i-PrOH (v/v = 1:1) under ambient conditions, is described. The chiral aryl N-heteroaryl methanols were obtained with up to 98.2% ee by introducing an N-oxide as a removable ortho-substituent. In contrast, no more than 15.1% ee was observed in the absence of an N-oxide moiety. Furthermore, the practical utility of this protocol was also demonstrated by gram-scale asymmetric synthesis of bepotastine besilate in 51% total yield and 99.9% ee.
Iron-catalyzed C-H bond functionalization for the exclusive synthesis of pyrido[1,2-a]indoles or triarylmethanols
Karthikeyan, Iyyanar,Sekar, Govindasamy
supporting information, p. 8055 - 8063 (2015/01/09)
The efficient and selective iron-catalyzed C-H activation of 2-benzhydrylpyridine derivatives was employed for the preparation of pyrido[1,2-a]indoles through an intramolecular C-H amination reaction. In the presence of molecular oxygen as the sole oxidant, the same 2-benzhydrylpyridines were also used for the synthesis of the corresponding tertiary alcohols. In these approaches, the iron catalyst was used to selectively activate the C(sp2)-H bond of 2-benzhydrylpyridine, in the case of the intramolecular ring-closing C-H amination reaction in which the pyridine nitrogen atom was a directing group as well as a nucleophile, and the C(sp3)-H bond of the same compound, in the case of the oxidation reaction to give the corresponding triaryl carbinol.
Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists
Cameron, Kimberly O.,Beretta, Elena E.,Chen, Yue,Chu-Moyer, Margaret,Fernando, Dilinie,Gao, Hua,Kohrt, Jeffrey,Lavergne, Sophie,Jardine, Paul Da Silva,Guzman-Perez, Angel,Hoth, Christopher,Perry, David A.,Hadcock, John R.,Gautreau, Denise,Makowski, Michael,Perez, Sylvie,Polivkova, Jana,Rogers, Lucy,Scott, Dennis O.,Swick, Andrew G.,Thiede, Lucinda,Trebino, Catherine E.,Trilles, Richard V.,Wilmowski, Julie,Zhang, Yingxin
supporting information; experimental part, p. 2943 - 2947 (2012/06/04)
New cholecystokinin-1 receptor (CCK1R) agonist 'triggers' were identified using iterative library synthesis. Structural activity relationship studies led to the discovery of compound 10e, a potent CCK1R agonist that demonstrated robust weight loss in a di
1,2,4 TRIAZOLO [4, 3 -A] [1,5] BENZODIAZEPIN-5 (6H) -ONES AS AGONISTS OF THE CHOLECYSTOKININ-1 RECEPTOR (CCK-IR)
-
Page/Page column 55-56, (2010/07/02)
This invention relates to CCK-1 R agonists of Formula (I) wherein R1-R5 and X are as defined in the specificiation, as well as pharmaceutical compositions containing the compounds and methods of use of the compounds and compositions. The compounds are useful in treating obesity, type 2 diabetes and associated diseases.
