357-60-8

Upstream product

• 579-39-5 1,2-bis(4-fluorophenyl)ethane-1,2-dione 
• 1693-26-1 1,1,1,2-tetrachloro-2,2-bis-(4-fluoro-phenyl)-ethane 
• 565-04-8 α,α,α',α'-tetrachloro-4,4'-difluoro-bibenzyl 

Downstream Products

• 379-59-9 4,4'-difluoro-benzilic acid ethyl ester 
• 207516-58-3 methyl 4,4'-difluorobenzilate 
• 762300-03-8 N-{3-[1-(3-{[bis(4-fluorophenyl)(hydroxy)acetyl]amino}propyl)-4-piperidinyl]-4-methylphenyl}-2-methylpropanamide 
• 762300-11-8 N-{5-[1-(3-{[bis(4-fluorophenyl)(hydroxy)acetyl]amino}propyl)-4-piperidinyl]-2,4-difluorophenyl}-2-methylpropanamide 
• 762300-50-5 N-{5-[1-(3-{[bis(4-fluorophenyl)(hydroxy)acetyl]amino}propyl)-4piperidinyl]-3-pyridinyl}-2-methylpropanamide 

Relevant academic research and scientific papers

PROCESS FOR THE PREPARATION OF SUBSTITUTED BENZILIC ACID FROM SUBSTITUTED BENZILS

The classical process for the rearrangement of substituted benzil to benzilic acid is performed in the presence of sodium or potassium hydroxide as a base using ethanol-ether as a medium. The reaction requires reflux temperature for complete conversion. However, these bases containing metallic ions and generate metallic containing effluent waste which may require additional expenditure for treatment. Moreover, because of corrosive nature of base, and use of flammable solvent, the safety measures are needed during large scale production. Another method also reported for benzilic acid rearrangement at 380° C. which is practically not feasible. The present invention describes the use of quaternary ammonium hydroxides as a base for the rearrangement of the substituted benzils to benzilc acids. It also avoids the use of solvent and reaction can be carried out at relatively lower temperatures. Because of the solvent free reaction condition it reduces the mass/volume of reaction mixture.

MEDICAMENTS FOR INHALATION COMPRISING ANTICHOLINERGICS AND A BETAMIMETIC

The present invention relates to novel pharmaceutical compositions comprising one or more, preferably one anticholinergic 1 and a betamimetic of formula 2 processes for preparing them and their use in the treatment of respiratory complaints.

SUBSTITUTED AZABICYCLO HEXANE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS

This invention relates to derivatives of substituted azabicyclo hexanes.The compound of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors.The invention also relates to a process for the preparation of compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.

3,6-DISUBSTITUTED AZABICYCLO [3.1.0] HEXANE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS

The invention relates to derivatives of 3,6-disubstituted azabicyclo [3.1.0] hexanes of structure (I). The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.

3,6-DISUBSTITUTED AZABICYCLO [3.1.0]HEXANE DERIVATIVES USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS

This invention generally relates to the derivatives of 3,6 disubstituted azabicyclo[3.1.0]hexanes. The compounds of this invention are muscarinic receptor antagonists which are useful, inter-alia, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.

Anticholinergics, processes for the preparation thereof, and pharmaceutical compositions

A compound of formula 1 wherein: X? is an anion with a single negative charge; A and B, which are identical or different, are each —O—, —S—, —NH—, —CH2—, —CH═CH—, or —N(C1-C4-alkyl)-; R is hydrogen, hydroxy, —C1-C4-alkyl, —C1-C4-alkyloxy, —C1-C4-alkylene-halogen, —O—C1-C4-alkylene-halogen, —C1-C4-alkylene-OH, —CF3, —CHF2, —C1-C4-alkylene-C1-C4-alkyloxy, —O—COC1-C4-alkyl, —O—COC1-C4-alkylene-halogen, —C1-C4-alkylene-C3-C6-cycloalkyl, —O—COCF3, or halogen; R1 and R2, which are identical or different, are each —C1-C5-alkyl, which is optionally substituted by —C3-C6-cycloalkyl, hydroxy, or halogen, or R1 and R2 together are a —C3-C5-alkylene bridge; R3, R4, R3′, and R4′, which are identical or different, are each hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, —CF3, —CHF2, —CN, —NO2, or halogen; Rx and Rx′, which are identical or different, are each hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, —CF3, —CHF2, —CN, —NO2, or halogen, or Rx and Rx′ together are a single bond or a bridging group selected from —O—, —S—, —NH—, —CH2—, —CH2—CH2—, —N(C1-C4-alkyl)-, —CH(C1-C4-alkyl)-, and —C(C1-C4-alkyl)2-, or a pharmacologically acceptable acid addition salt thereof, processes for preparing, them and their use in pharmaceutical compositions.