4479-75-8Relevant academic research and scientific papers
Convenient synthesis of various substituted homotaurines from alk-2-enamides
Nai, Youfeng,Xu, Jiaxi
, p. 1355 - 1365 (2013/08/23)
Various substituted homotaurines (=3-aminopropane-1-sulfonic acids) 6 were readily synthesized in satisfactory to good yields via the Michael addition of thioacetic acid to alk-2-enamides 3 (→4), followed by LiAlH4 reduction (→5) and performic acid oxidation (Scheme 1). The configuration of 'anti'-disubstituted homotaurine 'anti'-6h was deduced from the 3-(acetylthio)alkanamide (=S-(3-amino-1,2-dimethyl-3-oxopropyl) ethanethioate)'anti'-4h formed in the Michael addition, which was identified via the Karplus equation analysis, and confirmed by X-ray diffraction analysis. The current route is an efficient method to synthesize diverse substituted homotaurines, including 1-, 2-, and N-monosubstituted, as well as 1,2-, 1,N-, 2,N-, and N,N-disubstituted homotaurines (Table). Copyright
Fast and efficient one step synthesis of dienamides
Mathieson, Jennifer E.,Crawford, James J.,Schmidtmann, Marc,Marquez, Rodolfo
experimental part, p. 2170 - 2175 (2009/09/04)
A fast and efficient one-step approach to the synthesis of dienamides is reported. This concise methodology relies on the use of imides as reactive intermediates and allows for the preferential formation of Z,E-dienamides in good yields.
Analogs of isovaleramide, a pharmaceutical composition including the same, and a method of treating central nervous system conditions or diseases
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Page/Page column 6-7, (2010/02/15)
An isovaleramide analog having at least one of an increased potency, an increased half-life, and an increased stability compared to isovaleramide. The isovaleramide analog is a cyclic analog or a noncyclic analog. The isovaleramide analog is formulated into a pharmaceutical composition. A method of treating a central nervous system condition or disease is also disclosed. The method comprises administering an isovaleramide analog to a patient suffering from the central nervous system condition or disease.
PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF
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Page/Page column 112, (2010/02/12)
The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted C1-6 alkylene group etc.; Z represents -RB, -CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.,; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc., pharmaceutically acceptable salts thereof or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT1 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, impaired glucose tolerance, impaired fasting glycemia, diabetic complications or obesity, and a disease associated with the increase of blood galactose level such as galactosemia, and pharmaceutical compositions comprising the same, pharmaceutical uses thereof, and intermediates for production thereof.
Conformational Analysis of Some Acrylamide Homologues
Wojcik, Jacek,Szymanski, Slawomir,Witanowski, Michal,Stefaniak, Lech
, p. 613 - 619 (2007/10/02)
UV absorption and 13C NMR spectra of some acrylamide homologues are discussed in terms of their conformations.They usually assume the planar s-cis conformations, but steric effects in N,N-dimethylamides of methacrylic and senecioic acids are shown to force the molecules into non-planar structures.
