98572-00-0Relevant articles and documents
Lipase-catalyzed kinetic resolution of (±)-2-hydroxymethyl-1,4-benzodioxane
Antus,Gottsegen,Kajtar,Kovacs,Toth,Wagner
, p. 339 - 344 (1993)
The title compound has been kinetically resolved in a lipase-catalyzed transesterification with vinyl acetae in organic solvents. The influence of the enzyme source as well as the character of the solvent on the enantioselectivity has been studied.
Method for synthesizing optically pure 2-hydroxymethyl-1,4-benzodioxin and derivatives of optically pure 2-hydroxymethyl-1,4-benzodioxin
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Paragraph 0030-0032; 0034; 0035-0038, (2019/06/30)
The invention discloses a method for synthesizing optically pure 2-hydroxymethyl-1,4-benzodioxin and derivatives of the optically pure 2-hydroxymethyl-1,4-benzodioxin. The method comprises the steps that cheap 2-bromophenol or derivatives of the 2-bromoph
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles
Guo, Bin,Guo, Shimeng,Huang, Jing,Li, Jingya,Li, Jia,Chen, Qian,Zhou, Xianli,Xie, Xin,Yang, Yushe
, p. 5780 - 5791 (2018/11/06)
GPR40 has become a new potential therapeutic target for the treatment of diabetes due to its role in mediating the enhancement of glucose-stimulated insulin secretion in pancreatic β cells with a low risk of hypoglycemia. As an effort to extend the chemical space and identify structurally distinct GPR40 agonists with improved liver safety, a novel series of fused-ring phenyl propanoic acid analogues were designed. Comprehensive structure-activity relationship studies around novel scaffolds were conducted and led to several analogues exhibited potent GPR40 agonistic activities and high selectivity against other fatty acid receptors. Further evaluation of pharmacokinetic (PK) profiles and in vivo efficacy identified compound 40a with excellent PK properties and significant glucose-lowering efficacy during an oral glucose tolerance test. In addition, compound 40a displayed lower hepatobiliary transporter inhibition and favorable druggability. All results indicate that compound 40a is a promising candidate for further development.