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US 10,538,536 B2Granted
Process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one compounds
AssigneeHoffmann-La Roche Inc.
InventorsPascal Dott, Fabian Feyen, Stefan Hildbrand, Ursula Hoffmann, Fabienne Hoffmann-Emery, Roland Meier, Gerard Moine, Pankaj Rege, Georg Wuitschik
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Abstract
The present invention relates to a process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.
Claims19
A process for the preparation of compound of formula (I):
- which comprises reacting compound of formula (II):
- with a compound of formula (III):
- wherein
- R1 is hydrogen, C1-7-alkyl, or C3-8-cycloalkyl;
- R2 is hydrogen, halo, C1-7-alkyl, C1-7-haloalkyl or C3-8-cycloalkyl;
- R3 is hydrogen or C1-7-alkyl;
- R4 is C1-7-alkoxy;
- A is
- R5 to R8 are each independently selected from hydrogen and C1-3-alkyl.
6 more elements
A compound of formula (II):
- wherein,
- R1 is hydrogen, C1-7-alkyl, or C3-8-cycloalkyl;
- R2 is hydrogen, halo, C1-7-alkyl, C1-7-haloalkyl or C3-8-cycloalkyl;
- R3 is hydrogen or C1-7-alkyl;
- A is
- R5 to R8 are each independently selected from hydrogen and C1-3-alkyl.
3 more elements
A compound of formula (V):
- wherein
- R2 is hydrogen, halo, C1-7-alkyl, C1-7-haloalkyl or C3-8-cycloalkyl;
- R3 is hydrogen or C1-7-alkyl.
A compound of formula (II′):
A compound of formula (IV′):
A solid form of a compound of formula (I′) or a salt thereof
- characterized by an XRPD diffraction pattern comprising an XRPD peak at an angle of diffraction 2Theta at about 10.3°, 12.3°, 13.3°, and 15.4° (±0.2°).
A solid form of a compound of formula (I′) or a salt thereof
- characterized by an XRPD diffraction pattern comprising an XRPD peak at an angle of diffraction 2Theta at about 8.0°, 9.1°, 15.0°, and 23.7° (±0.2°).
Dependencies are inferred from the claim text.