78968-26-0

Upstream product

• 17094-34-7 ethyl pivaloylacetate 
• 81569-29-1 ethyl 2-bromo-4,4-dimethyl-3-oxopentanoate 
• 17356-08-0 thiourea 
• 29509-07-7 2-chloro-4,4-dimethyl-3-oxopentanoic acid ethyl ester 

Downstream Products

• 81569-31-5 ethyl 2-bromo-4-t-butylthiazole-5-carboxylate 
• 72850-77-2 Ethyl-2-chlor-4-t-butyl-5-thiazolcarboxylat 
• 81569-33-7 2-bromo-4-t-butylthiazole-5-carboxylic acid 

Relevant academic research and scientific papers

NF-KB ACTIVATION INHIBITORS

A medicament having inhibitory activity against NF-κB activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is 1○ a fused polycyclic heteroaryl group wherein the ring which binds directly to ―CONH― group in the formula (I) is a benzene ring, 2○ unsubstituted thiazol-2-yl group, or 3○ unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula ―O―A wherein A has the same meaning as that defined above and the group represented by formula -CONH-E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula ―O―A wherein A has the same meaning as that defined above and the group represented by formula ― CONH―E wherein E has the same meaning as that defined above.

THERAPEUTIC AGENT FOR CANCER

A medicament for the prevention and/or treatment of cancers and the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is 1? a fused polycyclic heteroaryl group wherein the ring which binds directly to ―CONH― group in the formula (I) is a benzene ring, 2? unsubstituted thiazol-2-yl group, or 3? unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula ―O―A wherein A has the same meaning as that defined above and the group represented by formula ―CONH―E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula ―O―A wherein A has the same meaning as that defined above and the group represented by formula ― CONH―E wherein E has the same meaning as that defined above.

REMEDIES FOR NEURODEGENERATIVE DISEASES

A medicament for preventive and/or therapeutic treatment of neurodegenerative diseases such as Alzheimer's disease or the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein A represents hydrogen atom or acetyl group, E represents a 2,5-di-substituted or a 3,5-di-substituted phenyl group, or a monocyclic or a fused polycyclic heteroaryl group which may be substituted, provided that the compound wherein said heteroaryl group is 1○ a fused polycyclic heteroaryl group wherein the ring which binds directly to -CONH- group in the formula (I) is a benzene ring, 2○ unsubstituted thiazol-2-yl group, or 3○ unsubstituted benzothiazol-2-yl group is excluded, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -CONH-E wherein E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -CONH-E wherein E has the same meaning as that defined above.

INHIBITORS AGAINST THE ACTIVATION OF AP-1 AND NFAT

A medicament inhibiting the activation of AP-1 which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula -O-A wherein A has the same meaning as that defined above and the group represented by formula -X-E wherein each of X and E has the same meaning as that defined above.

INHIBITORS AGAINST THE PRODUCTION AND RELEASE OF INFLAMMATORY CYTOKINES

A medicament having inhibitory activity against NF- κ B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.

Syntheses and Reactions of 2-Halo-5-thiazolecarboxylates

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.

The Preparation of Thiazole-4- and -5-carboxylates, and an Infrared Study of their Rotational Isomers

Convenient general procedures have been developed for preparing series of thiazole-4- and -5-carboxylates containing alkyl and halogeno substituents.While both series of esters show i.r. carbonyl doublets caused by rotational isomerism, the more intense absorptions of the 4-carboxylates are the lower wavenumber components, whereas those of the 5-carboxylates are the higher wavenumber components.In both series the stronger bands arise from the thermochemically more stable forms; identification of these forms as the carbonyl O,S-syn-s-trans rotamers is more certain with the 4-carboxylates than with the 5-carboxylates.

2-Amino-4-substituted-thiazolecarboxylic acids and their derivatives

2-Amino-4-substituted-5-thiazolecarboxylic acids and derivatives thereof, are intermediates for the preparation of 2-substituted-4-substituted-5-thiazolecarboxylic acid derivatives which are herbicidal safeners.