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US 2025/0066313 A1Published application
Methods of Synthesis of Chiral 3,5-Disubstituted Morpholine Compounds and Intermediates Useful Therein
OwnerYuanming Sun, Qin Zhang +4inventors
InventorsYuanming Sun, Qin Zhang, Jianzhang Yang, Zhongmin Xu, Xinzhong Lai, Joerg Deerberg
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Abstract
Provided herein are diastereomer-selective synthetic methods and intermediates for making chiral 3,5-disubstituted morpholine compounds, which are useful for the preparation of compounds useful as mitochondrial-derived activator of caspases (SMAC) mimetics for the treatment of proliferative diseases such as cancer.
Claims30
A compound of Formula (VI),
- or a pharmaceutically acceptable salt, solid form, enantiomer, isotopologue, or solvate thereof,
- wherein
- R1 and R2 are independently unsubstituted or substituted C1-5 alkyl.
(canceled)
A method for preparing a compound of Formula (VIII):
- or a pharmaceutically acceptable salt, solid form, enantiomer, isotopologue, or solvate thereof,
- wherein the method comprises contacting a compound of Formula (VII):
- with hydrogen (H2) in the presence of a catalyst in a solvent, wherein
- R1 and R2 are independently unsubstituted or substituted C1-5 alkyl.
1 more element
Dependencies are inferred from the claim text.