Reaktion #807300

Reaktionsgleichung

Intermediate 73(d)

N[2-(3-Dimethylaminomethyl-phenyl)-6-oxo-5,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl]-2-fluoro-3-trifluoromethyl-benzamide

(1R,2R)-2-phenyl-cyclopropanecarboxylic acid

triethylamine

O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate

→

title compound

Ausbeute 76.1%

(1R,2R)-2-phenyl-cyclopropanecarboxylic acid[2-(3-dimethylaminomethyl-phenyl)-6-oxo-5,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-yl]-amide

Ausbeute 76.1%

Lösungsmittel

N,N-dimethylformamide

isopropyl alcohol

CH2Cl2

Reaktionsbedingungen

Vorschrift

Preparation of example 83a from Intermediate 73(d) of Example 73 (0.11 g, 0.33 mmol), (1R,2R)-2-phenyl-cyclopropanecarboxylic acid (0.08 g, 0.5 mmol), triethylamine (0.183 mL, 1.32 mmol), O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (0.188 g, 0.5 mmol) and N,N-dimethylformamide (0.2 M, 1.7 mL) was carried out analogously to Example 11. Silica gel chromatography (90:10 to 80:20 CH2Cl2/2M ammonia in isopropyl alcohol) afforded the title compound (0.12 g) as powder in 76% yield.

Quelle