87848-95-1

Basic information

• Product Name: 6-BROMO-2-PYRIDYL P-TOLYL KETONE
• Synonyms: 6-BROMO-2-PYRIDYL P-TOLYL KETONE;2-Bromo-6-(4-methylbenzoyl) pyridine
• CAS NO: 87848-95-1
• Molecular Formula: C₁₃H₁₀BrNO
• Molecular Weight: 276.13
• Mol File: 87848-95-1.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• Density: 1.53 at 20℃
• Vapor Pressure: 0.002Pa at 25℃
• CAS DataBase Reference: 6-BROMO-2-PYRIDYL P-TOLYL KETONE(CAS DataBase Reference)
• NIST Chemistry Reference: 6-BROMO-2-PYRIDYL P-TOLYL KETONE(87848-95-1)
• EPA Substance Registry System: 6-BROMO-2-PYRIDYL P-TOLYL KETONE(87848-95-1)

Safety Data

• Hazardous Substances Data: 87848-95-1(Hazardous Substances Data)

Usage

Uses

(6-Bromopyridin-2-yl)(p-tolyl)methanone is an intermediate used in the synthesis of acrivastine; an antihistamine drug.

Upstream product

• 598-30-1 sec.-butyllithium 
• 74-11-3 para-chlorobenzoic acid 
• 74-88-4 methyl iodide 
• 626-05-1 2,6-Dibromopyridine 
• 104-85-8 para-methylbenzonitrile 

Downstream Products

• 87848-98-4 ethyl (E)-3-<6-<(4-methylphenyl)carbonyl>-2-pyridinyl>propeboate 
• 87848-96-2 2-(6-bromo-2-pyridyl)-2-(4-tolyl)-1,3-dioxolan 
• 87848-97-3 6-(2-p-Tolyl-[1,3]dioxolan-2-yl)-pyridine-2-carbaldehyde 
• 87848-99-5 acrivastine 

Relevant articles and documents

Triprolidine radioimmunoassay: Disposition in animals and humans

A hapten derivative of triprolidine, bearing an acrylic acid side chain ortho to the pyridine ring nitrogen atom, was synthesized and coupled to bovine serum albumin. Immunization of New Zealand White rabbits with the resulting drug-protein conjugate resulted in the production of antisera capable of binding a radioiodinated tyramine conjugate of the triprolidine hapten derivative at high antiserum dilutions (1:70,000-1:150,000). These antisera were used to develop a radioimmunoassay (RIA) for triprolidine in human plasma with a sensitivity limit of 0.1 ng/mL (0.01 ng of actual mass). The known hydroxymethyl and carboxyl metabolites of triprolidine cross-reacted weakly (2 and 0.05%, respectively) with this antiserum. The RIA could be used for the direct analysis of triprolidine in human and rabbit plasma, but not for rat or dog plasma, presumably due to the presence of other interfering substances (possibly metabolites). The validity of the RIA procedure in human plasma was demonstrated by comparative analysis of a number of samples by quantitative TLC (r = 0.985, slope = 1.076). The assay was employed to describe the pharmacokinetics of triprolidine in the rabbit (t( 1/2 ,β) = 1.7 h). The assay had adequate sensitivity to detect low circulating drug concentrations in humans after therapeutic oral doses and also substantiated previous disposition experiments with triprolidine in humans (t( 1/2 ,β = 2.27 h). TLC analysis demonstrated that the absolute oral bioavailability of triprolidine (1-mg/kg dose) in the dog was low (4%). A comparison of triprolidine pharmacokinetic parameters in dogs, rabbits, rats, and human revealed considerable similarity in elimination characteristics in these species.

TREATMENT OF CNS DISORDERS USING CNS TARGET MODULATORS

The invention is directed to compositions used for treating Central Nervous System (CNS) disorders. In addition, the invention provides convenient methods of treatment of a CNS disorder. Furthermore, the invention provides methods of treating sleep disorders using compositions that remain active for a discrete period of time to reduce side effects. More specifically, the invention is directed to the compositions and use of derivatized, e.g., ester or carboxylic acid derivatized, antihistamine antagonists for the treatment of sleep disorders.

3-{6-[3-Pyrrolidino-1-(4-tolyl)prop-1-enyl]-2-pyridyl}acrylic acid and pharmaceutically acceptable salts thereof

This disclosure describes a compound of Formula I STR1 (including its pharmaceutically acceptable salts and esters) which has potent antihistamine activity which is substantially free from sedative effects and which has little or no anticholinergic effects.