FIELD: chemistry.
SUBSTANCE: invention relates to a process for the preparation of (R)-5-bromo-4-(3-amino)piperidin-1-yl)-3-(cyclopropanecarboxamido)-1H-pyrrolo[2,3-b]pyridine of Formula (I): (I) or a pharmaceutically acceptable salt thereof, comprising reacting a compound of Formula (II):
(II), wherein X is halogen, with a compound of Formula (III):
(III), where R is an amino protecting group, to give a compound of Formula (IV):
(IV), nitro-reduction reaction of the compound of Formula (IV) to obtain a compound of Formula (V):
(V), reacting a compound of Formula (V) with a compound of Formula (VI):
(VI), where R1 is selected from the group consisting of chlorine, fluorine, bromine and OR2, where R2 is selected from the group consisting of cyclopropylcarbonyl, isobutylcarbonyl, isopropylcarbonyl, ethylcarbonyl, methylcarbonyl, 2-pyridyl and N-succinimidyl to give the compound of Formula (VII):
(VII) step of deprotecting R in the compound of Formula (VII) with pouring (R)-5-bromo-4-(3-(amino)piperidin-1-yl)-3-(cyclopropanecarboxamido)-1H-pyrrolo[2,3-b]pyridine of Formula (I).
EFFECT: method of preparing a compound is provided.
20 cl, 2 ex
Authors
Dates
2018-11-19—Published
2014-08-21—Filed