- An improved synthesis of 5-fluorothiophene-2-carboxylic acid
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A new and efficient route to 5-fluorothiophene-2-carboxylic acid 1 was secured in two steps and 62% yield overall.
- Chambers,Marfat
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- INHIBITOR OF CASEIN KINASE 1DELTA AND CASEIN KINASE 1E
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There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an act ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom).
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Paragraph 0091
(2013/06/05)
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- Thiophene and bioisostere derivatives as new MMP12 inhibitors
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A new MMP12 inhibitor series has been identified containing a thiophene moiety. Different approaches have been considered to replace this potential toxicophore. α-Fluorothiophene derivatives were the most interesting compounds. Their synthesis is presente
- Badland, Matthew,Compre, Delphine,Courté, Karine,Dublanchet, Anne-Claude,Blais, Stéphane,Manage, Ajith,Peron, Guillaume,Wrigglesworth, Roger
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scheme or table
p. 528 - 530
(2011/02/27)
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- OPIOID RECEPTOR ANTAGONISTS
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A compound of the formula I: (I) wherein the variables are as described herein, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixture thereof, formulations and methods of use thereof are disclosed.
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- Processes and intermediates for preparing 2-fluorothiophene derivatives
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PCT No. PCT/IB98/00304 Sec. 371 Date Jul. 26, 1999 Sec. 102(e) Date Jul. 26, 1999 PCT Filed Mar. 9, 1998 PCT Pub. No. WO98/45282 PCT Pub. Date Oct. 15, 1998A process for the preparation of the compound of the formula wherein R1 is OH, which comprises the steps of a) treating the compound of the formula with an inorganic fluoride, of the formula M2F wherein M2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R4P+Z- and a compound of the formula R5vic (COW)2 wherein R4 and R5 are each selected from optionally substituted (C6-C10)aryl and optionally substituted (C1-C6)alkyl, and W is halo; to form the compound of the formula; and b) i) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, and ii) treating the product of step i) with a mineral acid. A compound of the formula wherein R1 is selected from the group consisting of, halo, R7O, R7COO and N(R8)2 wherein R7 is (C1-C6)alkyl or (C6-C10)aryl and each R8 is selected from hydrogen and R7 with the proviso that R7 is not methyl when R1 is R7O.
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- Processes and intermediates for preparing 2-fluorothiophene derivatives
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A process for the preparation of the compound of the formula: wherein R1 is OH, which comprises the steps of a) treating the compound of the formula: with an inorganic fluoride, of the formula M2F wherein M2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R4P+Z- and a compound of the formula R5vic (COW)2 wherein R4 and R5 are each selected from optionally substituted (C6-C10) aryl and optionally substituted (C1-C6) alkyl, and W is halo; to form the compound of the formula: and b) I) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, and ii) treating the product of step i) with a mineral acid. A compound of the formula: wherein R1 is selected from the group consisting of, halo, R7O, R7COO and N(R8)2 wherein R7 is (C1-C6)alkyl or (C6-C10)aryl and each R8 is selected from hydrogen and R7 with the proviso that R7 is not methyl when R1 is R7O.
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