365996-05-0Relevant articles and documents
Novel 5,6,7,8-tetrahydroimidazo[2′,1′:2,3]thiazolo[5,4-c]pyridine derivatives
Hou, Xixi,Yang, Jianxue,Mao, Linlin,Lou, Caoxuan,Mao, Longfei
, p. 291 - 294 (2016)
Starting with 4-piperidone, new 5,6,7,8-tetrahydroimidazo[2′,1′:2,3]thiazolo [5,4-c]pyridines were synthesized. Structures of these compounds were confirmed by 1H NMR, 13C NMR, MS and elemental analysis.
Identification of novel GPR81 agonist lead series for target biology evaluation
Davidsson, ?jvind,Nilsson, Kristina,Br?nalt, Jonas,Andersson, Terese,Berggren, Kristina,Chen, Yantao,Fjellstr?m, Ola,Gradén, Henrik,Gustafsson, Linda,Hermansson, Nils-Olov,Jansen, Frank,Johannesson, Petra,Ohlsson, Bengt,Tyrchan, Christian,Wellner, Annika,Wellner, Eric,?lweg?rd-Halvarsson, Maria
supporting information, (2020/01/22)
GPR81 is a novel drug target that is implicated in the control of glucose and lipid metabolism. The lack of potent GPR81 modulators suitable for in vivo studies has limited the pharmacological characterization of this lactate sensing receptor. We performed a high throughput screen (HTS) and identified a GPR81 agonist chemical series containing a central acyl urea scaffold linker. During SAR exploration two additional new series were evolved, one containing cyclic acyl urea bioisosteres and another a central amide bond. These three series provide different selectivity and physicochemical properties suitable for in-vivo studies.
Preparation 2 - amino - 5 - CBZ - 4, 5, 6, 7 - tetrahydro-thiazolo [5, 4 - C] pyridine of the new method (by machine translation)
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Paragraph 0012; 0014, (2019/01/23)
The invention discloses a process for preparing 2 - amino - 5 - CBZ - 4, 5, 6, 7 - tetrahydro-thiazolo [5, 4 - C] pyridine of the new method, comprises the following steps: N - tert-butoxycarbonyl - 4 - piperidone in pyridine with sulfur and single cyanamide mixed heating reaction→cooling→filtering→washed with an organic solvent, and dried to obtain a pale yellow solid product→in dichloromethane in trifluoroacetic acid is mixed with low-temperature reaction, concentrated→with triethylamine in dichloromethane in the mixed low-temperature drop chlorination benzyl formate, stirring reaction→[...]→dichloromethane extraction, the organic phase water, salt water washing, drying, filtering and concentrated to obtain crude product→ethyl acetate beating, the final product is obtained yellow solid. The invention of cheap price for raw materials to replace the original high price of the raw material for preparing the final product, to avoid the original ring-brominated by-product when many routes, not only the operation is simple, convenient purification, the cost is reduced, high yield, favorable to the industrialized production and cost control. (by machine translation)