Réaction #2467944

ord-06a8605dd28f452196db886c1e1db1ac

Équation de réaction

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

Solvants

Conditions de réaction

Température
25°CELSIUS
Conditions détaillées
See reaction.notes.procedure_details.

Traitement

  1. 1
    Concentrationconcentrated in vacuo
  2. 2
    workup.DISSOLUTIONthe residue was dissolved in CH2Cl2 (20 mL)
  3. 3
    Lavagewas washed with 5% NaHCO3
  4. 4
    Séchagedried with MgSO4
  5. 5
    Concentrationconcentrated in vacuo
  6. 6
    AutreThe residue was purified by HPLC
  7. 7
    AutreThe product was obtained 170 mg (67%) as white solid

Mode opératoire

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.

Source

DOI: 10.6084/m9.figshare.5104873.v1Brevet: US08257931B2uspto-grants-2012_09