Реакция #3706

ord-27feefa6854942528e6b616195b74210

Уравнение реакции

[Na].c1nc[nH]n1
1,2,4-triazole sodium
O=C(CCl)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
2-chloro-N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)phenyl]acetamide
O=C(Cn1cncn1)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
desired product
Выход 64.5%
O=C(Cn1cncn1)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1
N-[4-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)phenyl]-2-(1H-[1,2,4]-triazol-1-yl)acetamide
Выход 64.5%

Условия реакции

Подробные условия
See reaction.notes.procedure_details.

Обработка

  1. 1
    ДругоеThe reaction mixture is quenched with 15 ml of water
  2. 2
    Другоеthe resulting solid is collected
  3. 3
    Промывкаwashed with water and hexanes

Методика

To a suspension of 0.20 g of 1,2,4-triazole sodium in 1 ml of 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone is added 0.10 g of 2-chloro-N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)phenyl]acetamide in 1 ml of 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone followed by stirring at room temperature for 3 hours. The reaction mixture is quenched with 15 ml of water and the resulting solid is collected, washed with water and hexanes to give 70 mg of the desired product as a tan solid. MS(CI): 413 (M+H).

Источник

DOI: 10.6084/m9.figshare.5104873.v1Патент: US05733905uspto-grants-1998_03