Application of 2-(2-difluoromethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborane_Kain Industrial Additive

Background and Overview

2-(2-Difluoromethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborane is an organic intermediate commonly used in metal catalysis coupling reaction,

Application examples^[1-2]

Report 1,

CN201780052527.0 reported that 2-(2-difluoromethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborane can be used to synthesize compound 6-amino -N-(5-chloro-6-(2-(difluoromethyl)phenyl)pyridin-2-yl)pyridine-2-sulfonamide. This compound is a CF transmembrane conductance regulator (CFTR) corrector. Cystic fibrosis (CF) is caused by loss-of-function mutations in the CF transmembrane conductance regulator (CFTR) protein, which is a cAMP-regulated chloride channel that is mainly found in the airways, pancreas, intestine and other tissues. Expressed in the apical serosa of secretory epithelium. CFTR is a large multi-domain glycoprotein consisting of two transmembrane domains, two nucleotide-binding domains (NBD1 and NBD2) that bind and hydrolyze ATP, and a regulatory (R) structure through a phosphorylation-gated channel Domain composition. The compounds may be used to prevent the onset of symptoms or complications of cystic fibrosis (CF), alleviate symptoms or complications, or eliminate the disease, condition or disorder.

Report 2,

CN201580038280.8 reported that 2-(2-difluoromethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborane can be used to prepare compounds [1- [5-[2-(Difluoro-methyl)-phenyl]-pyrimidin-2-yl]-spiro[1,2-dihydro-indole-3,1′-cyclopropane]-6-yl] -Morpholin-4-yl-methanone. Such compounds are selective PDE4B inhibitors and are particularly suitable for the treatment of diseases and conditions in which inhibition of PDE4 enzymes (especially PDE4B enzymes) is beneficial.

Main reference materials

[1] [Chinese invention] CN201780052527.0 N-(pyridin-2-yl)pyridine-sulfonamide derivatives and their use for disease treatment

[2] [Invented in China] CN201580038280.8 New substituted pyrimidine compound