Diisopropylethylamine → HCID 44540317, Verbindung

To a solution of 5-bromo-2-pyridinecarboxylic acid (980 mg, 4.83 mmol, available from Alfa Aesar) in DMF (15 ml) was added HATU (1840 mg, 4.83 mmol) and DIPEA (2.53 ml, 14.50 mmol). The mixture was stirred at room temperature for 30 mins then 6-(1H-indol-4-yl)-1H-indazol-4-amine (600 mg, 2.41 mmol) was added and the mixture stirred at room temperature overnight. The reaction mixture was concentrated in vacuo to approx. 5 ml volume and was applied to 2×50 g aminopropyl cartridges that had been pre-conditioned with MeOH. The reaction mixture remained on the cartridges for 2 h before being eluted with MeOH. The eluent was concentrated in vacuo and a precipitate formed, which was collected by filtration to give the title compound (430 mg) as a yellow solid.

1. stirringthe mixture stirred at room temperature overnight
2. concentrationThe reaction mixture was concentrated in vacuo to approx. 5 ml volume
3. waitThe reaction mixture remained on the cartridges for 2 h
4. washbefore being eluted with MeOH
5. concentrationThe eluent was concentrated in vacuo
6. customa precipitate formed
7. filtrationwhich was collected by filtration

ORD-Eintrag

ord-a200f78a3806479c87cfb28b600280f6

Quelldatensatz

uspto-grants-2014_07

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US08765743B2