- Synthesis of 4-Methylimidazole-2-Carboxylic Acid
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4-Methylimidazole-2-carboxylic acid was synthesized from 4-methylimidazole with a total yield of 65% over four steps including an N-benzyl protection, acylation, debenzylation, and ester hydrolysis. The solvent, base, temperature, and reaction time are op
- Wang, Xianheng,Zhao, Changkuo,Gao, Lei,Zhou, Yiqi,Xu, Lang
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- CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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Paragraph 1411
(2018/04/17)
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- 4-alkyl-imidazole-2-carboxylic acid synthesizing method
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The invention provides a method for synthesizing 4-alkylimidazole-2-carboxylic acid I. The method comprises the steps of firstly, reacting 2-alkyl-imidazole II as a raw material with BnX in the presence of a base to generate a mixture of a pair of position isomers IIIa and IIIb; secondly, on the premise that the mixture is not separated, reacting the mixture with halogenated formate (i.e., XCOOR2) in the presence of a base to generate a pair of corresponding isomers IVa and IVb; thirdly, hydrogenating to remove a benzyl group V in the presence of a hydrogenation catalyst; and fourthly, in the presence of a base, hydrolyzing to obtain the desired product 4-alkylimidazole-2-carboxylic acid I. The reaction route is shown in the specification, wherein R1 is selected from hydrogen atom and lower alkyl groups such as methyl and ethyl and R2 is selected from C1-C6 alkyl, C1-C6 alkoxy substituted group, a phenyl group or a benzyl group. The method disclosed by the invention has ingenious concept, since an inexpensive reagent is used in the respective step, and the yield of each step is high, the final target product 4-alkylimidazole-2-carboxylic acid I can be obtained in efficiency, convenience and low cost.
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Paragraph 0028; 0030; 0035; 0036
(2017/01/26)
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- HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
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Page/Page column 278
(2015/07/07)
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- IMIDAZOLE CARBONYL COMPOUND
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To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.
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Page/Page column 33
(2010/09/17)
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