864750-70-9

Basic information

• Product Name: 1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate
• Synonyms: TD-4208;Revefenacin;Revefenacin / TD4208;GSK1160724;Revefenacin:TD-4208:GSK-1160724
• CAS NO: 864750-70-9
• Molecular Formula: C₃₅H₄₃N₅O₄
• Molecular Weight: 597.74702
• EINECS: -0
• Mol File: 864750-70-9.mol
• Article Data: 8

Chemical Properties

• Boiling Point: 777.5±60.0 °C(Predicted)
• Appearance: /
• Density: 1.26±0.1 g/cm3(Predicted)
• PKA: 13.34±0.70(Predicted)
• CAS DataBase Reference: 1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate(864750-70-9)
• EPA Substance Registry System: 1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate(864750-70-9)

Safety Data

• Hazardous Substances Data: 864750-70-9(Hazardous Substances Data)

Usage

Description

Revefenacin is a synthetic anticholinergic that is prescribed for the treatment of chronic obstructive pulmonary disease (COPD).

Uses

Revefenacin is used to treat chronic obstructive pulmonary disease (COPD), a long-term (chronic) lung disease that includes chronic bronchitis, emphysema, or both. It is an anticholinergic drug that helps the muscles around the airways in the lungs stay relaxed to prevent symptoms such as wheezing, coughing, chest tightness, and shortness of breath.

Brand name

Yupelri

Side effects

Common adverse reactions in clinical trials (1%-10%) were headache, nasopharyngitis, upper respiratory tract infection, back pain, bronchitis, dizziness, and hypertension.

Upstream product

• 171722-92-2 4-piperidyl N-(2-biphenyl)carbamate 
• 743460-48-2 biphenyl-2-ylcarbamic acid 1-[2-(methylamino)ethyl]piperidin-4-yl ester 
• 16173-52-7 4-formylbenzoyl chloride 
• 619-66-9 4-Carboxybenzaldehyde 
• 1182906-72-4 4-(chloromethyl)-N-(2-hydroxyethyl)-N-methylbenzamide 
• 1642-81-5 p-(chloromethyl)benzoic acid 
• 39546-32-2 4-carboxamidopiperidine 
• 743460-49-3 biphenyl-2-ylcarbamic acid 1-[2-((benzyloxycarbonyl)-N-methylamino)ethyl]piperidin-4-yl ester 
• 17337-13-2 [1,1'-biphenyl]-2-yl-isocyanate 
• 4727-72-4 1-benzyl-4-hydroxypiperidine 
• 864760-28-1 biphenyl-2-yl-carbamic acid 1-{2-[(4-formylbenzoyl)methylamino]ethyl}piperidin-4-yl ester 

Relevant articles and documents

Preparation methods of revefenacin intermediate and revefenacin

The invention relates to a synthesis method of a revefenacin intermediate, which specifically comprises the following steps: in a solvent, enabling piperidin-4-yl [1,1-biphenyl]-2-carbamate to react with methyl(2-oxyethyl) tert-butyl carbamate in the pres

New rafenacin intermediate, active electrophilic building block thereof and new preparation method of rafenacin

The invention provides a new rafenacin intermediate, an active electrophilic building block thereof and a new preparation method of rafenacin. The new rafenacin intermediate shown as the formula (II) is prepared by sequentially reacting N-methylethanolamine with a compound shown as a formula (III) and a compound shown as a formula (V), and the new rafenacin intermediate shown as the formula (II) is used for activating hydroxyl to prepare an active electrophilic block shown as a formula (VI) and then reacts with a compound shown as a formula (VII) to obtain the rafenacin shown as the formula (I). The synthetic route provided by the invention has the advantages of short reaction steps, low raw material cost, simple reaction operation, mild conditions, high conversion rate, high selectivity and convenient post-treatment, and is more suitable for industrial production.

PROCESS FOR PREPARING A BIPHENYL-2-YLCARBAMIC ACID

The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.