반응 #6976

반응 방정식

BOP reagent

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

cyclopropylmethyl amine

→

title compound

수율 83.0%

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

수율 83.0%

용매

EtOAc

DMF

반응 조건

후처리

1. 1
   기타The above reaction mixture
2. 2
   세척washed with 10% NaHCO3 (3×5 mL), and 10% LiCl (5 mL)
3. 3
   건조The organic layer was dried over Na2SO4
4. 4
   농축concentrated
5. 5
   기타the residue was purified by preparative HPLC

실험 절차

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.

출처