تفاعل #159693

معادلة التفاعل

N-(4-fluoro-2-methylphenyl)azetidin-3-amine

triethylamine

methyl 4-(1-(2,5-dichloronicotinamido)cyclopropyl)benzoate

→

title compound ( D168 )

methyl 4-(1-(5-chloro-2-(3-((4-fluoro-2-methylphenyl)amino)azetidin-1-yl)nicotinamido)cyclopropyl)benzoate

المذيبات

tetrahydrofuran methanol

ظروف التفاعل

المعالجة

1. 1
   أخرىThe residue obtained
2. 2
   أخرىafter solvent evaporation
3. 3
   أخرىwas purified by Biotage SNAP-Si (10 g) cartridge
4. 4
   غسيلeluting
5. 5
   غسيلwith eluting with a mixture dichloromethane/ethylacetate from 95/5 to 80/20
6. 6
   أخرىCollected fractions, after solvent evaporation

الإجراء التجريبي

To a solution of N-(4-fluoro-2-methylphenyl)azetidin-3-amine (D55) and triethylamine (0.14 ml, 1.04 mmol) in tetrahydrofuran/methanol (3 ml/1 ml) methyl 4-(1-(2,5-dichloronicotinamido)cyclopropyl)benzoate (D97) (253 mg, 0.693 mmol) was added and the resulting mixture was heated 24 h at 75° C. The residue obtained after solvent evaporation, was purified by Biotage SNAP-Si (10 g) cartridge eluting with eluting with a mixture dichloromethane/ethylacetate from 95/5 to 80/20. Collected fractions, after solvent evaporation afforded the title compound (D168) (105 mg).

المصدر