41533-75-9

Upstream product

• 7716-66-7 3-chloro-1,2-benzisothiazole 
• 117054-79-2 7-nitrobenzisothiazol-3(2H)-one 

Downstream Products

• 90407-29-7 7-nitro-3-amino-1,2-benzisotiazolo 
• 1427158-29-9 2-chloro-N-(3-chlorobenzo[d]isothiazol-7-yl)-5-(pivalamidomethyl)benzamide 
• 148193-31-1 3-chlorobenzo[d]isothiazol-7-amine 
• 1427158-67-5 2-chloro-5-(pivalamidomethyl)-N-(3-((4-(trifluoromethyl)phenyl)amino)benzo[d]isothiazol-7-yl)benzamide 

Relevant academic research and scientific papers

METHOD FOR PRODUCING 3-HALO-1,2-BENZISOTHIAZOLES

A method for producing a 3-halo-1,2-benzisothiazole represented by the general formula (2): wherein R1 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, an alkoxycarbonyl group having 2 to 5 carbon atoms, a nitro group or a halogen atom, and X is a halogen atom, the method characterized by reacting a 1,2-benzisothiazol-3-one represented by the general formula (1): wherein R1 is the same group as the R1 defined in the above general formula (2), with a thionyl halide in a polar solvent. The 3-halo-1,2-benzisothiazole obtainable according to the method of the present invention is suitably used as production raw materials and the like for a medicament and the like.

SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS AS mPGES-1 INHIBITORS

The present invention relates to bicyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)

Effect of nitro-substituton on the photochemistry of 3-piperidino-1,2-benzisothiazole derivatives: A mechanistic investigation

Photochemical isomerization of 3-piperidino-1,2-benzisothiazole (BIT)-benzothiazole (BT) was investigated. In particular, the effect of nitro-substitution on the benzene ring was selectively examined for the parent, 5-nitro-, and 7-nitro-derivatives. 3-Piperidino-BIT and nitro-3-piperidino-BIT isomerized irreversibly to the corresponding 2-piperidino-BT, and this reaction mechanism was investigated using density-functional theory (DFT) and time-dependent (TD)-DFT calculations. These calculations showed that this isomerization goes through an azirine intermediate. In addition, excitation wavelength effect demonstrates that isomerization occurs from the upper excited state of nitro-derivatives. The HOMO-LUMO transition has charge-transfer and photoinactive characters.

Processes for producing isothiazole derivatives

A method for producing a 1,2-benzisothiazole characterized by treating a 2-(alkylthio)benzaldehyde oxime with a halogen compound; a method for producing a 3-halo-1,2-benzisothiazole characterized by treating a 1,2-benzisothiazole with a halogenating agent; and a method for producing a 1-(1,2-benzisothiazol-3-yl)piperazine characterized by reacting the obtained 3-halo-1,2-benzisothiazoles with a piperazine. By the method of the present invention, 1,2-benzisothiazoles and 3-halo-1,2-benzisothiazoles, which are useful as intermediates for pharmaceutical compositions such as psychotropic agents, and 1-(1,2-benzisothiazole-3-yl)piperazines synthesized therefrom can be obtained in a high yield without using expensive starting materials by shorter and simpler process than conventional methods.