반응 #6966

ord-27b9e1260647442584ff0f4565e0531d

반응 방정식

O=C(O)c1ccc(F)c(O)c1
3-hydroxy-4-fluorobenzoic acid
NC1CC1
cyclopropylamine
CCN(CC)CC
triethylamine
On1nnc2ccccc21
HOBt
CCN=C=NCCCN(C)C
EDCI
O=C(NC1CC1)c1ccc(F)c(O)c1
3-hydroxy-4-fluoro-N-cyclopropylbenzamide
수율 61.5%

용매

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    추출extracted with ethyl acetate (3×20 mL)
  2. 2
    세척The extract was washed with water
  3. 3
    농축concentrated

실험 절차

To a mixture of 3-hydroxy-4-fluorobenzoic acid (1.56 g, 10 mmol), cyclopropylamine (0.6 g, 10.5 mmol), triethylamine (1.02 g, 10 mmol) and HOBt (0.3 g, 2 mol) in DMF (10 mL) was added EDCI (2.0 g, 10.5 mmol) at RT. The mixture was stirred at RT overnight. The mixture was diluted with water and extracted with ethyl acetate (3×20 mL). The extract was washed with water and concentrated to afford 3-hydroxy-4-fluoro-N-cyclopropylbenzamide as a solid (1.2 g, 61.5%).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07084160B2uspto-grants-2006_08