反应 #1135840

ord-dcb05d37169b4b01acecedf154b74170

反应方程式

Nc1ccccc1NC1CC1
N1-cyclopropylbenzene-1,2-diamine
CCN(CC)CC
triethylamine
COC(=O)CCCCCCC(=O)Cl
methyl 8-chloro-8-oxooctanoate
COC(=O)CCCCCCC(=O)Nc1ccccc1NC1CC1
methyl 8-(2-(cyclopropylamino)phenylamino)-8-oxooctanoate
收率 94.2%

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    洗涤washed with 1 N HCl, saturated sodium bicarbonate solution and brine
  2. 2
    浓缩The separated organic layer was concentrated

实验过程

To a solution of N1-cyclopropylbenzene-1,2-diamine (221 mg, 1.49 mmol) and triethylamine (0.3 mL, 2.2 mmol) in DMF was added a solution of methyl 8-chloro-8-oxooctanoate (260 mg, 1.3 mmol) in DMF at 0° C. drop-wise. The reaction was stirred overnight at room temperature, diluted with ethyl acetate and washed with 1 N HCl, saturated sodium bicarbonate solution and brine. The separated organic layer was concentrated to give crude methyl 8-(2-(cyclopropylamino)phenylamino)-8-oxooctanoate (390 mg)

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US09381196B2uspto-grants-2016_07