- AMINOPHENYLCYCLOPROPYL CARBOXYLIC ACIDS AND DERIVATIVES AS AGONISTS TO GPR40
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The present invention relates generally to novel therapeutic compounds and more particularly to novel compounds, their use as GPR40 agonists, processes for their manufacture, and intermediates useful in their preparation.
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Page/Page column 67
(2008/06/13)
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- 4-Chloro-5H-1,2,3-dithiazol-5-one: A good α-thiocyanating agent for α,β-unsaturated β-amino esters
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Treatment of 4-chloro-5H- 1,2,3-dithiazol-5-one with 3-alkyl (or aryl)- 3-amino-2-propenoate esters in DMSO at 120°C gave the corresponding 2- thiocyanated esters 4 (major) and 5-alkoxycarbonyl-4-alkyl (or aryl)-4- thiazolin-2-ones 5 (minor), whereas the
- Park, Young Seok,Kim, Kyongtae
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p. 6439 - 6442
(2007/10/03)
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- Pyrazolecarboxylic acid derivatives and plant disease control agent
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The present invention provides a plant disease control agent containing as active ingredient one or more compounds of the formula [1]A--COOR 1 [1]whereinR 1 represents a hydrogen atom or a C 1 -C 4 alkyl group, andA represents a group of the formula (A-1) or (A-2) STR1 R 2 represents a C 1 -C 4 alkyl group, R 3 represents a C 1 -C 4 alkyl group,R 4 represents a halogen atom or a C 1 -C 4 alkyl group, andR 5 represents a C 1 -C 4 alkyl group.Further, the compound of A-1 in the formula [1] in which R 3 is a halogen atom is also included in the present invention.
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- Pseudohalogen chemistry. XI. Some aspects of the chemistry of octhiocyanato-β-dicarbonyl compounds
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Enolised α-thiocyanato-β-dicarbonyl compounds dimerise in ethanol at room temperature to give tautomeric 4,5-disubstituted 2-amino- and 2-acetamido-thiazoles by a C-S-C + C-N cyclisation. Tautomerism is due to the unusual 4-(β-dicarbonyl-α-thio) substituent. Competing intramolecular cyclisations lead to minor amounts of heterocycles containing the thiazole and/or oxathiole ring systems.
- Atkins, Elaine F.,Dabbs, Steven,Guy, Robert G.,Mahomed, Akbar A.,Mountford, Philip
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p. 7253 - 7264
(2007/10/02)
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- Synthesis of Heterocyclic Compounds from 0-Aminobenzenethiol and Ammonium Thiocarbamate
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The reaction of o-aminobenzenethiol with carbonyl sulfide in the presence of triethylamine afforded an alternate route for the synthesis of 2-benzothiazolinone (1) in 97-98percent yield.The reaction of ammonium thiocarbamate (2) with 2-chlorocyclohexanone furnished the novel 4,5,6,7-tetrahydro-2-benzothiazolinone (3). 3-Ethoxy-2H-1,4-benzothiazin-2-one (7) was prepared by the reaction of o-aminobenzenethiol with diethyl oxalate.Possible pathways and supporting nmr, ir and mass spectra are discussed.
- D'Amico, John J.,Fuhrhop, Ralph W.,Bollinger, Frederic G.,Dahl, William E.
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p. 641 - 645
(2007/10/02)
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- Syntheses and Reactions of 2-Halo-5-thiazolecarboxylates
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A variety of 2-halo-5-thiazolecarboxylates was prepared from substituted-3-aminoacrylates and 3-ketoesters.Selective reduction of 2-chloro-5-thiazolecarboxylates 4a, 4i and 4j with sodium borohydride in ethanol provided the corresponding 2-halo-5-thiazolemethanols 27 - 29.Nucleophilic displacement on methyl methanesulfonate (32c) occured selectivity at the 5-substituent to provide 2-chloro-4-(trifluoromethyl)-5-(heteroatom-substituted methyl)thiazoles 32d-f.
- Lee, Len F.,Schleppnik, Francis M.,Howe, Robert K.
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p. 1621 - 1630
(2007/10/02)
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- Novel thiazole derivatives
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Novel compounds of the formula EQU1 wherein X is selected from the group consisting of oxygen and sulfur, X1 is selected from the group consisting of alkyl of 1 to 6 carbon atoms, cyano and EQU2 Y1 is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms and amino, n is 0, 1 or 2, X2 is selected from the group consisting of hydrogen, chlorine, bromine, alkyl of 1 to 6 carbon atoms, cyano and EQU3 R is alkyl of 1 to 6 carbon atoms, R1 is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms and EQU4 and R2 and R3 are selected from the group consisting of hydrogen and alkyl of 1 to 6 carbon atoms with the proviso that X1 is other than alkyl when X2 is alkyl or hydrogen, having insecticidal, nematocidal and acaricidal properties.
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- 2-Thiazolone-5-carboxylic acid ester fungicidal agents
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Fungicidal compositions containing, and methods of combating fungi using, 2-thiazolone-5-carboxylic acid ester fungicidal agents of the formula SPC1 In which R1 is hydrogen; alkyl of up to 12 carbon atoms optionally substituted by phenyl, halop
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