3,4-dihydro-2H-pyrano[2,3-c]pyridine-6-carbaldehyde → 3-Chloro-4-({(3r,4s)-4-[(3,4-dihydro-2h-pyrano[2,3-c]pyridin-6-ylmethyl)amino]-3-hydroxy-1-piperidinyl}methyl)-4,5-dihydro-7h-pyrrolo[3,2,1-de]-1,5-naphthyridin-7-one hydrochloride

Participants

Reaction Steps

The free base of the title compound was prepared from racemic 4-{[(3R,4S)-4-amino-3-hydroxy-1-piperidinyl]methyl}-3-chloro-4,5-dihydro-7H-pyrrolo[3,2,1-de]-1,5-naphthyridin-7-one and 3,4-dihydro-2H-pyrano[2,3-c]pyridine-6-carbaldehyde (for a synthesis see WO2004058144, Example 126(e)) according to the general method of Example 24(b), chromatographing with dichloromethane/methanol/0.88 ammonia 95:5:0.5, in 50% yield.

Provenance & Evidence