112498-22-3Relevant articles and documents
Efficient Generation of C–S Bonds via a By-Product-Promoted Selective Coupling of Alcohols, Organic Halides, and Thiourea
Ma, Xiantao,Yu, Lei,Su, Chenliang,Yang, Yaqi,Li, Huan,Xu, Qing
, p. 1649 - 1655 (2017)
A metal- and base-free three-component coupling of alcohols, heteroaryl halides, and thiourea has been developed for direct and selective synthesis of heteroaryl thioethers. This method can be easily scaled up to the gram scale and extended to dialkyl thioethers, heteroaryl selenides, benzothiazoles, and some antimycobacterially-active thioethers. Mechanistic studies revealed that a by-product-promoted in situ C–O activation of alcohols to more reactive alkyl halides and slow release of the thiol and alkyl halide intermediates are the key to the high selectivity and success of the reaction. (Figure presented.).
Exploration of pyrrole derivatives to find an effective potassium-competitive acid blocker with moderately long-lasting suppression of gastric acid secretion
Nishida, Haruyuki,Fujimori, Ikuo,Arikawa, Yasuyoshi,Hirase, Keizo,Ono, Koji,Nakai, Kazuo,Inatomi, Nobuhiro,Hori, Yasunobu,Matsukawa, Jun,Fujioka, Yasushi,Imanishi, Akio,Fukui, Hideo,Itoh, Fumio
supporting information, p. 3447 - 3460 (2017/05/29)
With the aim to discover a novel excellent potassium-competitive acid blocker (P-CAB) that could perfectly overcome the limitations of proton pump inhibitors (PPIs), we tested various approaches based on pyrrole derivative 1 as a lead compound. As part of a comprehensive approach to identify a new effective drug, we tried to optimize the duration of action of the pyrrole derivative. Among the compounds synthesized, fluoropyrrole derivative 20j, which has a 2-F-3-Py group at position 5, fluorine atom at position 4, and a 4-Me-2-Py sulfonyl group at the first position of the pyrrole ring, showed potent gastric acid-suppressive action and moderate duration of action in animal models. On the basis of structural properties including a slightly larger C?log?P value (1.95), larger log?D value (0.48) at pH 7.4, and fairly similar pKa value (8.73) compared to those of the previously optimized compound 2a, compound 20j was assumed to undergo rapid transfer to the stomach and have a moderate retention time there after single administration. Therefore, compound 20j was selected as a new promising P-CAB with moderately long duration of action.
Substituted pyridinesulfonamide compounds, and herbicidal compositions containing them
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, (2008/06/13)
A substituted pyridinesulfonamide compound having the formula (I): STR1 wherein R1 is an alkyl group, a haloalkyl group, an alkoxyalkyl group or an alkenyl group, R2 is a hydrogen atom, an alkyl group, a haloalkyl group, an alkoxyalk