反応 #6976

反応方程式

BOP reagent

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

cyclopropylmethyl amine

→

title compound

収率 83.0%

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

収率 83.0%

溶媒

EtOAc

DMF

反応条件

後処理

1. 1
   その他The above reaction mixture
2. 2
   洗浄washed with 10% NaHCO3 (3×5 mL), and 10% LiCl (5 mL)
3. 3
   乾燥The organic layer was dried over Na2SO4
4. 4
   濃縮concentrated
5. 5
   その他the residue was purified by preparative HPLC

実験手順

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.

出典