تفاعل #329299

معادلة التفاعل

2-chloro-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid chloride

3-fluorobenzylamine

DIPEA

→

2-chloro-N-(3-fluorobenzyl)-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid amide

المردود 97.0%

المذيبات

1,4-dioxane

1,4-dioxane

water

EA

ظروف التفاعل

المعالجة

1. 1
   أخرىThe organic phase was separated
2. 2
   غسيلwashed with a 4N aq. NH4Cl sol. and brine
3. 3
   تجفيفdried over MgSO4
4. 4
   تركيزconcentrated in a vacuum

الإجراء التجريبي

A solution of 15.6 g (50.6 mmol) 2-chloro-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid chloride in 1,4-dioxane (85 ml) was added in drops to a solution of 7.6 g (60.8 mmol) 3-fluorobenzylamine and 10.3 ml (60.8 mmol) DIPEA in 1,4-dioxane (87 ml). The RS was subsequently stirred for 60 min at RT. The solution was then diluted with water and EA. The organic phase was separated, washed with a 4N aq. NH4Cl sol. and brine, dried over MgSO4 and concentrated in a vacuum. 19.4 g (48.9 mmol, 97%) 2-chloro-N-(3-fluorobenzyl)-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid amide was obtained as a residue. The raw product was further converted without additional purification.

المصدر