1260670-71-0Relevant articles and documents
Sulfur-assisted ring contraction of polyfluoroalkylthiopyran derivatives as a route to functionalized fluorine-containing thiophenes
Siry, Sergiy A.,Timoshenko, Vadim M.,Schermolovich, Yuriy G.
, p. 17 - 21 (2016)
A synthetic route to functionalized α-(polyfluoroalkyl)thiophenes based on the reactions of ring contraction of polyfluoroalkyl substituted thiopyran derivatives has been explored. Potent 6-membered precursors for the preparation of thiophenes were obtained by the addition of bromine to the double bonds of 2-chloro-2-(trifluoromethyl)-3,6-dihydro-2H-tetrahydrothiopyran and 6-(polyfluoroalkyl)-2H-thiopyrans. The reactions of the resulted 4,5-dibromo-2-chloro-2-(trifluoromethyl)tetrahydrothiopyrans and trans-3,4-dibromo-6-(polyfluoroalkyl)-3,4-dihydro-2H-thiopyrans with sodium acetate in acetic acid produced 2-(acetoxymethyl)-5-(polyfluoroalkyl)thiophenes. Base-catalyzed methanolysis of the acetoxymethyl derivatives allowed preparing the corresponding 2-(hydroxymethyl)-5-(polyfluoroalkyl)thiophenes. The mechanism, which includes formation and nucleophilic cleavage of thiiranium cations, has been suggested for the transformation of dibromothiopyran derivatives to substituted thiophenes.
Triazinone compound and T-type calcium channel inhibitor
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Page/Page column 89; 90, (2016/08/29)
There is provided a novel triazinone compound that has an excellent T-type voltage-dependent calcium channel inhibitory activity and is specifically useful for treatment of pain. A compound of Formula (I), a tautomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof: where each substituent is defined in detail in the description or claims, for example R1 is H or C1-6 alkoxy, etc., each of L1 and L2 is independently a single bond or NR2, etc., L3 is C1-6 alkylene, etc., A is C6-14 aryl or 5 to 10-membered heteroaryl which is optionally substituted, etc., B is C3-11 cycloalkylene, etc., D is C6-14 aryl or 5 to 10-membered heteroaryl which is optionally substituted, etc.