反応 #2467944

ord-06a8605dd28f452196db886c1e1db1ac

反応方程式

CCOC(=O)C(Cc1ccccc1)C(=O)O
2-Benzyl-malonic acid monoethyl ester
CCN=C=NCCCN(C)C.Cl
1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride
Nc1nc(-c2ccccc2)cs1
4-phenyl-thiazol-2-ylamine
CCOC(=O)C(Cc1ccccc1)C(=O)Nc1nc(-c2ccccc2)cs1
2-Benzyl-N-(4-phenyl-thiazol-2-yl)-malonamic acid ethyl ester

溶媒

反応条件

温度
25°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    濃縮concentrated in vacuo
  2. 2
    workup.DISSOLUTIONthe residue was dissolved in CH2Cl2 (20 mL)
  3. 3
    洗浄was washed with 5% NaHCO3
  4. 4
    乾燥dried with MgSO4
  5. 5
    濃縮concentrated in vacuo
  6. 6
    その他The residue was purified by HPLC
  7. 7
    その他The product was obtained 170 mg (67%) as white solid

実験手順

To a suspension of 2-Benzyl-malonic acid monoethyl ester (150 mg, 0.67 mmol) and 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (0.74 mmol) in DMF (4 mL) at 25° C. was added 4-phenyl-thiazol-2-ylamine (119 mg, 0.67 mmol), the resulting mixture was stirring at 25° C. for overnight and concentrated in vacuo, and the residue was dissolved in CH2Cl2 (20 mL) was washed with 5% NaHCO3, dried with MgSO4 and concentrated in vacuo. The residue was purified by HPLC. The product was obtained 170 mg (67%) as white solid.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08257931B2uspto-grants-2012_09