743460-49-3

Usage

Uses

Used in Pharmaceutical Industry:
Biphenyl-2-ylcarbamic acid 1-[2-((benzyloxycarbonyl)-N-methylamino)ethyl]piperidin-4-yl ester is used as an intermediate in the synthesis of Des-4''(methylpiperidine-4-carboxamide)-4''-hydroxymethyl Revefenacin (D119860), an impurity of Revefenacin (R279600). Revefenacin is a pharmaceutical drug used for the treatment of chronic obstructive pulmonary diseases (COPD). biphenyl-2-ylcarbamic acid 1-[2-((benzyloxycarbonyl)-N-methylamino)ethyl]piperidin-4-yl ester's role in the synthesis process is essential for the development of effective treatments for this respiratory condition.
In the pharmaceutical industry, biphenyl-2-ylcarbamic acid 1-[2-((benzyloxycarbonyl)-N-methylamino)ethyl]piperidin-4-yl ester is utilized for its potential to contribute to the creation of new drug candidates. Its unique structure allows for the exploration of various chemical modifications, which can lead to the discovery of novel therapeutic agents with improved efficacy and safety profiles. biphenyl-2-ylcarbamic acid 1-[2-((benzyloxycarbonyl)-N-methylamino)ethyl]piperidin-4-yl ester's involvement in the synthesis of Revefenacin highlights its importance in the development of treatments for chronic obstructive pulmonary diseases, a significant health concern worldwide.

Upstream product

• 67580-96-5 benzyl (2-hydroxyethyl)methylcarbamate 
• 171723-80-1 1-benzyl-4-piperidylbiphenyl-2-ylcarbamate 
• 1355573-66-8 (2,2-Dimethoxyethyl)methylcarbamic Acid Benzyl Ester 
• 501-53-1 benzyl chloroformate 
• 17337-13-2 [1,1'-biphenyl]-2-yl-isocyanate 
• 4727-72-4 1-benzyl-4-hydroxypiperidine 
• 107201-33-2 N-<(benzyloxy)carbonyl>-N-methylaminoacetaldehyde 
• 171722-92-2 4-piperidyl N-(2-biphenyl)carbamate 

Downstream Products

• 864750-70-9 biphenyl-2-yl carbamic acid 1-(2-{[4-((4 carbamoylpiperidin-1-yl)methyl)benzoyl]N-methylamino}ethyl)piperidin-4-yl ester 
• 743460-48-2 biphenyl-2-ylcarbamic acid 1-[2-(methylamino)ethyl]piperidin-4-yl ester 

Relevant academic research and scientific papers

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

Discovery of (R)-1-(3-((2-Chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1′-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, Batefenterol): First-in-Class dual pharmacology multivalent muscarinic antagonist and β2 agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD)

Through application of our multivalent approach to drug discovery we previously reported the first discovery of dual pharmacology MABA bronchodilators, exemplified by 1. Herein we describe the subsequent lead optimization of both muscarinic antagonist and β2 agonist activities, through modification of the linker motif, to achieve 24 h duration of action in a guinea pig bronchoprotection model. Concomitantly we targeted high lung selectivities, low systemic exposures and identified crystalline forms suitable for inhalation devices. This article culminates with the discovery of our first clinical candidate 12f (TD-5959, GSK961081, batefenterol). In a phase 2b trial, batefenterol produced statistical and clinically significant differences compared to placebo and numerically greater improvements in the primary end point of trough FEV1 compared to salmeterol after 4 weeks of dosing in patients with moderate to severe chronic obstructive pulmonary disease (COPD).

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.

Compounds having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity

The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.