Reacción #3614

Ecuación de reacción

10,11-dihydro-10-(4-amino-3-methylbenzoyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine

N,N-diisopropylethylamine

2-methylbenzoyl chloride

→

solid

Rendimiento 65.9%

N-[4-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)-2-methylphenyl]-2-methylbenzamide

Rendimiento 65.9%

Disolventes

methylene chloride

Condiciones de reacción

Tratamiento posterior

1. 1
   LavadoThe reaction mixture is washed with water
2. 2
   Secadothe organic layer dried with Na2SO4
3. 3
   workup.ADDITIONHexane is added at the boil

Procedimiento

A solution of 0.83 g of 10,11-dihydro-10-(4-amino-3-methylbenzoyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine, 0.5 g of N,N-diisopropylethylamine and 0.6 g of 2-methylbenzoyl chloride in 50 ml of methylene chloride is stirred at room temperature for 18 hours. The reaction mixture is washed with water, the organic layer dried with Na2SO4 and passed through a pad of hydrous magnesium silicate. Hexane is added at the boil to give 0.75 g of a solid which is crystallized from methylene chloride-hexane to give 0.61 g of the desired product, m.p. 125°-130° C.

Fuente