7716-65-6

Upstream product

• 4163-04-6 3-chloro-2-phenyl-benzo[d]isothiazolium; chloride 
• 23564-81-0 N-phenyl-2-(2-chlorophenyl)formamidine 
• 873-32-5 2-Chlorobenzonitrile 
• 62-53-3 aniline 

Downstream Products

• 75190-37-3 2-Mercapto-N-phenylbenzamidin 

Relevant academic research and scientific papers

Discovery of a Potent and Orally Bioavailable Hypoxia-Inducible Factor 2α (HIF-2α) Agonist and Its Synergistic Therapy with Prolyl Hydroxylase Inhibitors for the Treatment of Renal Anemia

Activation of hypoxia-inducible factor 2 (HIF-2) has emerged as a potent renal anemia treatment strategy. Here, the benzisothiazole derivative 26 was discovered as a novel HIF-2α agonist, which first demonstrated nanomolar activity (EC50 = 490 nM, Emax = 349.2%) in the luciferase reporter gene assay. Molecular dynamics simulations indicated that 26 could allosterically enhance HIF-2 dimerization. Furthermore, compound 26 had a good pharmacokinetic profile (the oral bioavailability in rats was 41.38%) and an in vivo safety profile (the LD50 in mice was greater than 708 mg·kg-1). In the in vivo efficacy assays, the combination of 26 and the prolyl hydroxylase inhibitor, AKB-6548, was confirmed for the first time to synergistically increase the plasma erythropoietin level in mice (from 260 to 2296 pg·mL-1) and alleviate zebrafish anemia induced by doxorubicin. These results provide new insights for HIF-2α agonists and the treatment of renal anemia.

3 - Aminobenzo [d] isothiazole. Derivative and synthesis method thereof

The invention mainly relates to 3-aminobenzo[d]isothiazole and derivatives thereof and a synthetic method thereof. Benzamidine compounds and elemental sulfur are converted into 3-aminobenzo[d]isothiazole and the derivatives thereof only under the action of an alkali and in an air atmosphere without use of a catalyst during synthesis. The problems that a conventional synthetic method of a functionalized 3-aminobenzo[d]isothiazole compound has complex synthetic steps, requires a multistep synthesis process to complete, and also requires use of metal catalysts or peroxides, as well as has low yield or harsh reaction conditions are overcome. The synthetic method has the characteristics of simple reaction system, mild reaction conditions, less reaction equipment, simple experimental operation,wide sources of used materials, high yield, easy expanding of users and application, high utilization value of products, expectable prospects of commercialization of the market and the like.

Efficient synthesis of 1,2-benzisothiazoles from: O -haloarylamidines and elemental sulfur via N-S/C-S bond formation under transition-metal-free conditions

An efficient method for the synthesis of 1,2-benzisothiazoles from amidines and elemental sulfur via N-S/C-S bond formation under transition-metal-free conditions is described. This reaction is performed smoothly under simple conditions to give the corresponding products in good to high yields with good functional group tolerance.

Rearrangement Reactions of 2-Alkyl(Aryl)-3-arylimino-1,2-benzisothiazolines

3-Chloro-1,2-benzisothiazolium chlorides 1 react with aromatic amines to give the 2-substituted 3-arylimino-1,2-benzisothiazolines 2 which can rearrange to the isomeric 1,2-benzisothiazolines 3 in an equilibrium reaction.On a formal basis this entails an