Category: 72600-67-0

Ohmi, Masashi published the artcileIdentification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist, Safety of 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, the main research area is pyridylbenzensulfonamide derivative RQ00203078 preparation TRPM8 antagonist cold allodynia; structure activity TRPM8 antagonist pyridylbenzensulfonamide derivative RQ00203078; Cold allodynia; RQ-00203078; Sulfonamide; TRPM8 antagonist; Wet-dog shakes.

A novel series of 2-pyridyl-benzensulfonamide derivatives have been identified as selective and orally active TRPM8 antagonists via high throughput screening (HTS). Exploration of the structure-activity relationships of compound (I) has led to the identification of RQ-00203078 (compound 36) as a highly selective, potent and orally available TRPM8 antagonist. RQ-00203078 demonstrated excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration and may become an important pharmacol. tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation.

Bioorganic & Medicinal Chemistry Letters published new progress about Allodynia (cold). 72600-67-0 belongs to class pyridine-derivatives, name is 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, and the molecular formula is C6H2ClF4N, Safety of 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 72600-67-0, name is 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, molecular formula is C6H2ClF4N, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. COA of Formula: C6H2ClF4N

(c) 47.7 g (0.82 mol) of potassium fluoride and 10.0 g (0.065 mol) of caesium fluoride are suspended in 300 ml of sulfolane and the suspension is heated to 140 C. 60 ml of sulfolane are distilled off by decreasing the pressure and subsequently 65.6 g (0.329 mol) of 2-chloro-3-fluoro-5-trifluoromethylpyridine and 1.3 g (0.004 mol) of 18-crown-6 are added. The reaction mixture is stirred for 48 hours at 140 C. and subsequently distilled by introducing steam. The oil is separated and the aqueous phase is extracted twice with a small amount of ether. The organic phases are purified, dried with a small amount of magnesium sulfate and filtered. Distillation affords 54.8 g (91% of theory) of 2,3-difluoro-5-trifluoromethylpyridine, b.p. 100-102 C. (980 mbar).

With the rapid development of chemical substances, we look forward to future research findings about 72600-67-0.

Reference:
Patent; Ciba-Geigy Corporation; US4831148; (1989); A;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 72600-67-0, name is 2-Chloro-3-fluoro-5-(trifluoromethyl)pyridine, molecular formula is C6H2ClF4N, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. COA of Formula: C6H2ClF4N

(c) 47.7 g (0.82 mol) of potassium fluoride and 10.0 g (0.065 mol) of caesium fluoride are suspended in 300 ml of sulfolane and the suspension is heated to 140 C. 60 ml of sulfolane are distilled off by decreasing the pressure and subsequently 65.6 g (0.329 mol) of 2-chloro-3-fluoro-5-trifluoromethylpyridine and 1.3 g (0.004 mol) of 18-crown-6 are added. The reaction mixture is stirred for 48 hours at 140 C. and subsequently distilled by introducing steam. The oil is separated and the aqueous phase is extracted twice with a small amount of ether. The organic phases are purified, dried with a small amount of magnesium sulfate and filtered. Distillation affords 54.8 g (91% of theory) of 2,3-difluoro-5-trifluoromethylpyridine, b.p. 100-102 C. (980 mbar).

With the rapid development of chemical substances, we look forward to future research findings about 72600-67-0.

Reference:
Patent; Ciba-Geigy Corporation; US4831148; (1989); A;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem