反应详情

0.5 g (1.85 mmol) of (R)-1-(2-azido-propyl)-7-methoxy-1,4-dihydro-indeno[2,1-c]pyrazole dissolved in 50 ml of anhydrous ethanol were hydrogenated over 50 mg of platinum oxide for 2 hours. The catalyst was subsequently filtered off, rinsed with ethanol and the solvent was removed in a vacuum. The colorless oil obtained was dissolved in 70 ml of anhydrous diethyl ether, filtered and treated while stirring with a solution of 215 mg(1.85 mmol) of fumaric acid in 5 ml of methanol. The mixture was stirred at room temperature for 15 hours and the white crystals were subsequently filtered off. 0.55 g (83%) of (R)-2-(7-methoxy-1,4-dihydro-indeno[2,1-c]pyrazol-1 -yl)-1-methyl-ethylamine fumarate (1:1) with m.p. 180° was obtained.

1. filtrationThe catalyst was subsequently filtered off
2. washrinsed with ethanol
3. customthe solvent was removed in a vacuum
4. customThe colorless oil obtained
5. filtrationfiltered
6. additiontreated
7. filtrationthe white crystals were subsequently filtered off