65214-82-6Relevant articles and documents
Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes
Pola, Suresh,Shah, Shailesh R.,Pingali, Harikishore,Zaware, Pandurang,Thube, Baban,Makadia, Pankaj,Patel, Hoshang,Bandyopadhyay, Debdutta,Rath, Akshyaya,Giri, Suresh,Patel, Jitendra H.,Ranvir,Sundar,Patel, Harilal,Kumar, Jeevan,Jain, Mukul R.
, (2021/03/30)
The ever-growing prevalence of Type-2 diabetes in the world has an urgent need for multiple orally effective agents that can regulate glucose homeostasis. G-Protein coupled receptor 119 (GPR 119) agonists have demonstrated the glucose-dependent insulin secretion and showed beneficial effects on glycemic control in humans and/or relevant animal models. Herein, we describe our efforts towards identification of a potent and oral GPR 119 agonist 13c (ZY-G19), which showed in vitro potency in the cell-based assay and in vivo efficacy without exerting any significant signs of toxicity in relevant animal models.
Synthesis method of N-ethoxycarbonyl-4-hydroxypiperidine
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Paragraph 0018; 0020; 0023; 0026, (2018/05/16)
The invention discloses a synthesis method of N-ethoxycarbonyl-4-hydroxypiperidine and belongs to the technical field of organic chemistry. In the presence of a catalytic amount of ammonium chloride,4-hydroxypiperidine is added to hexamethyldisilazane for a reflux reaction, 4-trimethylsiloxypiperidine is obtained, an intermediate and diethyl carbonate are subjected to a sealed reaction at the high temperature, and N-ethoxycarbonyl-4-hydroxypiperidine is obtained. The method has the characteristics that raw materials are easy to obtain, the cost is low, factory operation is simple and convenient and the yield is high. In synthesis, highly toxic ethyl chloroformate is not used, and a method is provided for synthesis of the compound.
Development of two diastereoselective routes towards trans-4-aminomethyl-piperidin-3-ol building blocks
Gijsen, Harrie J.M.,De Cleyn, Michel J.A.,Love, Christopher J.,Surkyn, Michel,Van Brandt, Sven F.A.,Verdonck, Marc G.C.,Moens, Luc,Cuypers, Jef,Bosmans, Jean-Paul R.M.A.
, p. 2456 - 2464 (2008/09/18)
Two diastereoselective, scaleable routes towards trans-3,4-disubstituted piperidines with a 4-hydroxymethyl-3-hydroxy or 4-aminomethyl-3-hydroxy substitution pattern are being described. In the first route, the 3,4-trans configuration was introduced regio- and diastereoselectively via a hydroboration/oxidation sequence starting from 4-hydroxymethylpyridine. In the second route, regioselective epoxide ring opening of N-benzyl-3,4-epoxy-piperidine was achieved with LiCN, in situ generated from acetocyanohydrin and LiNH2. The regioselectivity of both the hydroboration and the epoxide ring opening was positively influenced by the presence of the basic piperidine nitrogen. Both routes have been optimized to be performed at large scale.
