Reaktion #807308

Reaktionsgleichung

title compound

8-Amino-2-phenyl-1,5-dihydro-[1,2]diazepino[4,5,6-cd]indol-6-one

(R)-tert-butoxycarbonylamino-3-phenyl-propionic acid

triethylamine

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

→

title compound

Ausbeute 110.7%

[(R)-1-(6-Oxo-2-phenyl-5,6-dihydro-1H-[1,2]diazepino[4,5,6-cd]indol-8-ylcarbamoyl)-2-phenyl-ethyl]-carbamic acid tert-butyl ester

Ausbeute 110.7%

Lösungsmittel

CH2Cl2

N,N-dimethylformamide

Reaktionsbedingungen

Aufarbeitung

1. 1
   WaschenSilica gel chromatography (eluted with 1:1 hexane:acetone)

Vorschrift

Preparation of example 118 from the title compound of Example 7 (hydrochloride) (43 mg, 0.138 mmol), (R)-tert-butoxycarbonylamino-3-phenyl-propionic acid (44 mg, 0.166 mmol), triethylamine (0.058 mL, 0.414 mmol), and O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (63 mg, 0.166 mmol) in CH2Cl2 (0.4 mL) and N,N-dimethylformamide (0.4 mL) was carried out analogously to Example 11. Silica gel chromatography (eluted with 1:1 hexane:acetone), also in an analogous manner, afforded the title compound (80 mg) as a yellow powder contaminated with an unknown impurity. The compound was carried on without further purification to Example 115.

Quelle