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US 2021/0147417 A1Published application
Processes for preparing an fgfr inhibitor
AssigneePrincipia Biopharma Inc.
InventorsJiang ZHU, Mohammad MASJEDIZADEH
Life of this patent
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Abstract
Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.
Claims21
-18. (canceled)
A process of preparing a compound of formula (a):
- comprising reacting a compound of formula (5) with a compound of formula (i) where X is a leaving group under elimination reaction conditions and LG is either a leaving group under acylation reaction conditions or a hydroxy
- group to give the compound of formula (a).
A process of preparing a compound of formula (b):
- comprising reacting a compound of formula (5) with an alkyne of formula (ii) where LG1 is either a leaving group under acylation conditions or a hydroxyl group
- to give the compound of formula (b).
(canceled)
An intermediate of formula (6-1):
- or a salt thereof, where:
- both R are either hydrogen or chloro;
- and
- X is halo, phosphate, tosylate, or mesylate.
1 more element
A crystalline free base, an amorphous free base, a crystalline hydrochloride salt, or a crystalline maleate salt of a compound of formula:
(canceled)
(canceled)
(canceled)
Dependencies are inferred from the claim text.