52179-07-4Relevant articles and documents
Microwave-assisted synthesis, hypolipidemic and hypoglycemic activity of some novel 2-(4-(2-amino-6-(4-substituted phenyl)-pyrimidin-4-yl)-phenoxy)-2- methyl propanoic acid derivatives
Mokale, Santosh N.,Elgire, Rupali D.,Sakle, Nikhil S.,Shinde, Devanand B.
experimental part, p. 22 - 27 (2012/03/10)
A novel series of aminopyrimidines containing the phenoxy isobutyric acid group as a pharmacophore was synthesized using conventional and microwave assisted methods of synthesis. The compounds were synthesized in good yields (70-89%) by the microwave-assisted one-pot protocol in much shorter reaction times. The synthesized compounds were evaluated for their hypolipidemic and hypoglycemic activity by high-fat diet-induced hyperlipidemia and hyperglycemia in male Sprague-Dawley rats. The present investigation showed significant antihyperlipidemic and antihyperglycemic activity for all compounds of the series when compared with the standard drug. Structure-activity relationship (SAR) for the series were developed by comparing total lipid profile data of synthesized compounds with fenofibrate as standard drug. A novel series of aminopyrimidines containing the phenoxy isobutyric acid group as a pharmacophore was synthesized using conventional and microwave-assisted methods of synthesis. The synthesized compounds were evaluated for their hypolipidemic and hypoglycemic activities on high-fat diet-induced hyperlipidemia and hyperglycemia in male Sprague-Dawley rats. Copyright
Degradation Studies under Neutral and Basic Conditions on Ciprofibrate, an Orally Active Hypolipidemic Agent Containing a (4-Alkoxyaryl)-1,1-dichlorocyclopropane Unit
Dulayymi, Juma'a R. Al,Baird, Mark S.,Byard, Stephen J.,Carr, Glynis,Ellames, George J.,et al.
, p. 43 - 48 (2007/10/02)
The major product of degradation of ciprofibrate (1), 2-(4-(2,2-dichlorocyclopropyl)phenoxy>-2-methylpropanoic acid, in aqueous sodium hydroxide under reflux is 2--2-methylpropanoic acid (11).A further product, 2-(4-ethynylphenoxy)-2-methylpropanoic acid (12) is derived from 11 under the reaction conditions.A third degradant is identified as 2--2-methylpropanoic acid (13).Under similar conditions, but at pH 7, the products of degradation were found to be2--2-methylpropanoic acid (9) and (Z)-2--2-methylpropanoic acid (10).Treatment of 10 with aqueous sodium hydroxide under reflux afforded a mixture of products in which 11 and 12 predominated, whereas similar treatment of 9 led to compound 13 among other products.A labelling study indicates that the acid 21 derived from base treatment of 17 is labelled only at C-2 of the propanoic acid side chain; the same labelling pattern is observed in the acid 21 derived by base treatment of the labelled allylic alcohol 18.Mechanisms are suggested which may explain these observations.
