反应详情

To a solution of (3-(5-chloro(3-pyridyloxy))-1-methylpropyl)methylamine (0.70 g, 3.27 mmol) in ethanol (20 mL) at 70° C. was added galactaric acid (0.343 g, 1.63 mmol). Water (0.5 mL) was added drop-wise while stirring, producing a clear solution. Some white, insoluble solids were removed by filtration. The filtrate was concentrated to 10 mL and was allowed to cool to ambient temperature. After standing 16 h, the precipitate was filtered, washed with ether (10 mL) and vacuum dried at 45° C. for 24 h to give 0.775 g (74.3%) of a light-beige, amorphous powder, mp 155-157° C. The compound exhibits a Ki of 1601 nM. The compound exhibits neurotransmitter release of 30 percent.

1. customproducing a clear solution
2. customSome white, insoluble solids were removed by filtration
3. concentrationThe filtrate was concentrated to 10 mL
4. filtrationthe precipitate was filtered
5. washwashed with ether (10 mL) and vacuum
6. customdried at 45° C. for 24 h
7. customto give 0.775 g (74.3%) of a light-beige, amorphous powder, mp 155-157° C