تفاعل #41743

معادلة التفاعل

2-{[4-bromo-3-fluorophenylamino)-1-methylbenzimidazol-5-yloxy)pyridine-2-carboxylic acid

2-piperidylethylamine

HBTU

N,N-diisopropylethylamine

→

4-(2-{[4-bromo-3-fluorophenyl]amino-1-methylbenzimidazol-5-yloxy)(2-pyridyl)]-N-(2-piperidylethyl)carboxamide

المذيبات

tetrahydrofuran

ظروف التفاعل

المعالجة

1. 1
   تركيزThe mixture was then concentrated
2. 2
   أخرىpartitioned between ethyl acetate and water
3. 3
   تركيزThe organic layer was concentrated

الإجراء التجريبي

To 4-(2-{[4-bromo-3-fluorophenylamino)-1-methylbenzimidazol-5-yloxy)pyridine-2-carboxylic acid (1 eq) in tetrahydrofuran was added 2-piperidylethylamine (2 eq), HBTU (2 eq) and N,N-diisopropylethylamine (4 eq) and stir at ambient temperature for 16 h. The mixture was then concentrated and partitioned between ethyl acetate and water. The organic layer was concentrated and preparative chromatography yielded [4-(2-{[4-bromo-3-fluorophenyl]amino-1-methylbenzimidazol-5-yloxy)(2-pyridyl)]-N-(2-piperidylethyl)carboxamide. MS: MH+=567.

المصدر