Реакция #6976

Уравнение реакции

BOP reagent

4-fluoro-3-{[2-(pyridin-2-ylamino)-thiazol-5-ylmethyl]-amino}-benzoic acid

cyclopropylmethyl amine

→

title compound

Выход 83.0%

N-Cyclopropylmethyl-4-fluoro-3-{[2-(pyridin-2-ylamino)-thiazol-5-ylmethyl]-amino}-benzamide

Выход 83.0%

Растворители

EtOAc

DMF

Условия реакции

Обработка

1. 1
   ДругоеThe above reaction mixture
2. 2
   Промывкаwashed with 10% NaHCO3 (3×5 mL), and 10% LiCl (5 mL)
3. 3
   СушкаThe organic layer was dried over Na2SO4
4. 4
   Концентрированиеconcentrated
5. 5
   Другоеthe residue was purified by preparative HPLC

Методика

To a solution of 4-fluoro-3-{[2-(pyridin-2-ylamino)-thiazol-5-ylmethyl]-amino}-benzoic acid (35 mg, 0.10 mmol) in DMF (1 mL) at RT, cyclopropylmethyl amine (14 mg 0.20 mmol) was added followed by the addition of BOP reagent (53 mg, 0.12 mmol). The above reaction mixture was stirred for 2 h, diluted with EtOAc (10 mL), washed with 10% NaHCO3 (3×5 mL), and 10% LiCl (5 mL). The organic layer was dried over Na2SO4, concentrated and the residue was purified by preparative HPLC to give the title compound as a off-white solid (33 mg, 83%). (M+H)+=398.

Источник