862574-87-6

Usage

Uses

Used in Medicinal Chemistry:
1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarbonitrile is used as a starting material for the synthesis of other organic compounds, particularly in the field of medicinal chemistry. Its unique structure, including the cyclopropane ring and the difluorobenzo[d][1,3]dioxol-5-yl moiety, may offer advantages in the development of new pharmaceutical agents.
Due to the complex nature and potential reactivity of 1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarbonitrile, it necessitates careful handling and further research to fully understand its properties and explore its potential applications. This may include evaluating its stability, reactivity, and compatibility with other compounds in various chemical reactions and synthesis processes.

Upstream product

• 68119-31-3 2-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)acetonitrile 
• 107-04-0 1-Bromo-2-chloroethane 
• 33070-32-5 5-bromo-2,2-difluoro-2H-1,3-benzodioxole 
• 656-46-2 2,2-difluoro-1,3-benzodioxole-5-carboxylic acid 
• 72768-97-9 (2,2-difluoro-1,3-benzodioxol-5-yl)methanol 
• 476473-97-9 5-chloromethyl-2,2-difluoro-benzo[1,3]dioxole 
• 1335233-51-6 (2,2-difluoro-1,3-benzodioxol-5-yl)-1-ethylacetate acetonitrile 
• 14866-33-2 tetraoctyl ammonium bromide 
• 1583-59-1 2,2-difluoro-1,3-benzodioxole 
• 773873-95-3 2,2-difluorobenzo[1,3]dioxole-5-carboxylic acid methyl ester 
• 1634-04-4 tert-butyl methyl ether 

Downstream Products

• 1152311-62-0 (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide 
• 1294504-68-9 N-{1-[(2R)-3-(benzyloxy)-2-hydroxypropyl]-2-[1-(benzyloxy)-2-methylpropan-2-yl]-6-fluoro-1H-indol-5-yl}-1-(2,2-difluoro-2H-1,3-benzodioxol-5-yl)cyclopropane-1-carboxamide 
• 1152274-48-0 2-(3-(3-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropane carboxamido)isoquinolin-1-yl)benzoyloxy)-N,N,N-trimethylethanaminium chloride 
• 1152274-36-6 2-(dimethylamino)ethyl 3-(3-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)isoquinolin-1-yl)benzoate 
• 1152274-55-9 tert-butyl 3-(3-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)isoquinolin-1-yl)benzoate 
• 1152274-47-9 1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(4-(hydroxymethyl)phenyl)isoquinolin-3-yl)cyclopropanecarboxamide 
• 1152274-56-0 3-(3-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)isoquinolin-1-yl)benzoyl chloride 
• 1083168-21-1 N-(6-(1-(2-cyanamido-2-oxoethyl)-6-oxo-1,6-dihydropyridin-3-yl)-5-methylpyridin-2-yl)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamide 
• 1083168-23-3 1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(6-(5-fluoro-2-oxo-1,2-dihydropyridin-4-yl)-5-methylpyridin-2-yl)cyclopropanecarboxamide 
• 1160221-26-0 Lumacaftor hydrochloride 
• 936727-05-8 Lumacaftor 
• 1160221-25-9 tert-butyl 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropane-1-carboxamido)-3-methylpyridin-2-yl)benzoate 
• 862574-88-7 1-(2,2-difluorobenzo[1,3]dioxol-5-yl)cyclopropane-1-carboxylic acid 

Relevant academic research and scientific papers

Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases

The present invention features compositions comprising a plurality of therapeutic agents wherein the presence of one therapeutic agent enhances the properties of at least one other therapeutic agent. In one embodiment, the therapeutic agents are cystic fibrosis transmembrane conductance regulators (CFTR) such as a CFTR corrector or CFTR potentiator for the treatment of CFTR mediated diseases such as cystic fibrosis. Methods and kits thereof are also disclosed.

METHODS OF TREATMENT FOR CYSTIC FIBROSIS

This application describes methods of treating cystic fibrosis or a CFTR mediated disease comprising administering Compound I or a pharmaceutically acceptable salt thereof. (I) The application also describes pharmaceutical compositions comprising Compound I or a pharmaceutically acceptable salt thereof and optionally comprising one or more additional CFTR modulating agents.

METHODS OF TREATMENT FOR CYSTIC FIBROSIS

Compound I of the formula (I) and/or pharmaceutically acceptable salt(s) of Compound I comprised in a pharmaceutical composition and methods of using the same to treat cystic fibrosis.

1 - (2, 2 - Difluorobenzene and [D] [1, 3] dioxo heterocyclic pentene -5 - yl) ring propyl nitrile of preparation method

The invention discloses a preparation method for 1-(2,2-difluoro-benzo[D][1,3]dioxol-5-yl)-cyclopropanecarbonitrile. The method comprises the following steps: 5-(chloromethyl)benzo[d][1,3]dioxole is prepared from 2,2-difluoro-1,3-benzodioxole through Blanc chloromethylation, and then is subjected to cyanation by utilization of cuprous cyanide, finally cyclization is carried out by utilization of 1-Bromo-2-chloroethane and a product is obtained. In the above method, cyanation is carried out by utilization of low-toxic cuprous cyanide, a weak organic base triethylamine deacid reagent is employed to carry out cyclization preparation and a target product is obtained, usage of dangerous lithium aluminum hydride and sodium cyanide is avoided, strong alkaline and high temperature conditions are avoided, and therefore hydrolysis of cyan in the product is avoided. The preparation method is low-toxic to the environment and the product yield and quality are raised. The process flow is simple and safe, the reaction process is easy to control, the cost is low, the yield is high, and the preparation method is suitable for industrialization.

MODULATOR OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR, PHARMACEUTICAL COMPOSITIONS, METHODS OF TREATMENT, AND PROCESS FOR MAKING THE MODULATOR

Compounds of Formula (I) pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed. Also disclosed are solid state forms of Compound 1 and salts and solvates thereof.

PHARMACEUTICAL COMPOSITIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL)CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID AND ADMINISTRATION THEREOF

A pharmaceutical composition comprising Compound 1,(3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.

Efficient cyclopropanation of aryl/heteroaryl acetates and acetonitriles with vinyl diphenyl sulfonium triflate

A convenient method was developed for the cyclopropanation of aryl acetates and aryl acetonitrile using vinyl diphenyl sulfonium triflate salt. The newly developed conditions are simple, mild, and compatible with a wide range of functional groups, without the need to apply an inert atmosphere, or alkali bases.

FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID

A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a disintegrant, a surfactant, a binder, and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Processes of preparing pharmaceutical compositions comprising Compound 1 are also disclosed.

Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[D][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid and administration thereof

A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.

CYCLOPROPANECARBOXAMIDE MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.