24827-66-5

Upstream product

• 111248-89-6 1,3-dihydro-2,1-benzisothiazole 2,2-dioxide 
• 74-88-4 methyl iodide 
• 77421-13-7 (2-chlorobenzyl)sulfonyl chloride 
• 615-36-1 2-bromoaniline 
• 116547-91-2 N-(2-bromophenyl)methanesulfonamide 
• 553652-34-9 N-(2-bromophenyl)-N-methylmethanesulfonamide 
• 111249-29-7 2-aminobenzylsulfonic acid sodium salt 
• 89665-79-2 (2-chlorophenyl)-methanesulfonamide 

Downstream Products

• 187333-17-1 1-methyl-3-(4-nitrophenyl)-1,3-dihydro-2,1-benzisothiazole 2,2-dioxide 
• 57503-00-1 N-o-tolyl-methanimine 
• 623159-68-2 3-(3-chloro-4-nitrophenyl)-1-methyl-1,3-dihydro-2,1-benzisothiazole 2,2-dioxide 
• 5339-28-6 N-methyl-N-(2-vinylphenyl)amine 

Relevant academic research and scientific papers

Synthesis of Oxindole Derivatives via Intramolecular C–H Insertion of Diazoamides Using Ru(II)-Pheox Catalyst

This work presented the efficient intramolecular aromatic C–H insertion of diazoacetamide. The 1a–1o diazo compounds (except for 1k) were converted into their corresponding oxindoles via an intramolecular C–H insertion reaction in the presence of a Ru catalyst. The Ru-Pheox catalyst was shown to be highly efficient in this transformation in terms of the regioselectivity, producing the desired products in excellent yield (99%). The efficiency of the Ru catalyst reached 580 (TON) and 156 min?1 (TOF).

NOVEL NAPHTHYRIDINES AND ISOQUINOLINES AND THEIR USE AS CDK8/19 INHIBITORS

The present invention relates to naphthyridine and isoquinoline compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of CDK8/19, and for the treatment of CDK8/19-related disorders.

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in human disease, particularly in colorectal cancer where it has been reported as a putative oncogene. Here we report the discovery of 109 (CCT251921), a potent, selective, and orally bioavailable inhibitor of CDK8 with equipotent affinity for CDK19. We describe a structure-based design approach leading to the discovery of a 3,4,5-trisubstituted-2-aminopyridine series and present the application of physicochemical property analyses to successfully reduce in vivo metabolic clearance, minimize transporter-mediated biliary elimination while maintaining acceptable aqueous solubility. Compound 109 affords the optimal compromise of in vitro biochemical, pharmacokinetic, and physicochemical properties and is suitable for progression to animal models of cancer.

PYRIDYL PIPERIDINES

The invention provides novel substituted pyridyl piperidine compounds according to Formula (I) which are Wnt pathway inhibitors, their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.

2-AMINOPYRIDINE COMPOUNDS

The invention provides novel substituted 2-aminopyridine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.

Synthesis of spiropyrrolidinyl-benzoisothiazoline derivatives by 1,3-dipolar cycloaddition of benzoisothiazole-2,2-dioxide-3-ylidenes and azomethine ylide

The new spirocyclic compounds, spiropyrrolidinyl-benzoisothiazoline derivatives were synthesized by the 1,3-dipolar cycloaddition of benzoisothiazole-2,2-dioxide-3-ylidenes and azomethine ylide. The stereochemistry of 1,3-dipolar cycloaddition as well as the stereochemistry of Knoevenagel condensation of benzoisothiazole-2,2-dioxide with aldehydes were studied.

2,1-Benzisothiazoline 2,2-Dioxide and Derivatives

Synthesis of new 2,1-benzisothiazoline 2,2-dioxides 1 and some of its benzene ring substitution derivatives was accomplished by two different methods of cyclisation.Also a number of new N-substituted derivatives, obtained by treatment of 1 and analogues w