20660-73-5Relevant academic research and scientific papers
Design, synthesis, and pharmacological evaluation of fused β-homophenylalanine derivatives as potent DPP-4 inhibitors
Jiang, Tao,Zhou, Yuren,Chen, Zhuxi,Sun, Peng,Zhu, Jianming,Zhang, Qiang,Wang, Zhen,Shao, Qiang,Jiang, Xiangrui,Li, Bo,Chen, Kaixian,Jiang, Hualiang,Wang, Heyao,Zhu, Weiliang,Shen, Jingshan
supporting information, p. 602 - 606 (2015/05/27)
Dipeptidyl peptidase-4 (DPP-4) inhibitors are accepted as a favorable class of agents for the treatment of type 2 diabetes. Herein, a series of fused β-homophenylalanine derivatives as novel DPP-4 inhibitors were designed, synthesized, and evaluated for their inhibitory activities against DPP-4. Most of them displayed excellent DPP-4 inhibitory activities and good selectivity. Among them, 9aa, 18a, and 18m also showed good efficacy in an oral glucose tolerance test (OGTT) in ICR mice. Moreover, when dosed 8 h prior to glucose challenge, 18m showed significantly greater potency than sitagliptin. It thus provides potential candidates for the further development into potent drugs targeting DPP-4.
Benzylic brominations with N-bromosuccinimide in (Trifluoromethyl)benzene
Suarez, Diana,Laval, Gilles,Tu, Shang-Min,Jiang, Dong,Robinson, Claire L.,Scott, Richard,Golding, Bernard T.
experimental part, p. 1807 - 1810 (2010/02/28)
A variety of benzylic brominations were performed by using N-bromosuccinimide in (trifluoromethyl)benzene with photochemical activation in the presence of 2,2′-azobisisobutyronitrile, 1,1′- azobis(cyclohexanecarbonitrile), or benzoyl peroxide as the radical initiator. This system provides clean, rapid, and high-yielding reactions with replacement of conventional solvents, such as tetrachloromethane, by less-toxic (trifluoromethyl)benzene. Georg Thieme Verlag Stuttgart.
PYRROLO[2,3-C]PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 12-13, (2010/10/20)
The present invention provides novel pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect.
PYRROLO[2,3-c]PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 9, (2010/10/20)
The present invention provides novel pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[2,3-c]pyridine derivatives or pharmaceutically acceptable salts thereof of the present invention have excellent proton pump inhibition effects and possess the ability to attain a reversible proton pump inhibitory effect.
Pyridylcarbamates, process and intermediates for their preparation, and their use
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, (2008/06/13)
A pyridylcarbamate compound of the formula I STR1 wherein R' is hydrogen; opt. subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkylcarbonyl and alkoxycarbonyl; R" is opt. subst. alkyl, alkenyl, alkynyl, cycloalkyl and cycloalkenyl; or is hydrogen when V is nitrogen; V is O, S or N; X is cyano; nitro; halogen; opt. subst. alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, or an opt. subst. bridge which is bonded to two adjacent C atoms of the pyridyl ring; n is 0, 1, 2 or 3; R is halogen; OH; SH; NH; CHO; CO2 H; CONH2 ; opt. subst. alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl or hetaryl, each being bonded directly or via O, S, N, CO2 or CONH; or together with X and the pyridyl ring to which they are bonded an opt. subst. bicyclus, its manufacture, and pesticidal and fungicidal compositions containing I.
