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US 10,745,404 B2Granted
Process for the synthesis of E1 activating enzyme inhibitors
AssigneeMillennium Pharmaceuticals, Inc.
InventorsIan Armitage, Eric L. Elliott, Marianne Langston, Steven P. Langston, Quentin J. McCubbin, Hiro Mizutani, Matthew Stirling, Lei Zhu
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Abstract
The present invention provides processes and synthetic intermediate (Ia) for the synthesis of 4-substituted ((1S, 2S, 4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates. These sulfamate compounds are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.
Claims7
A compound of formula (Ia):
- or a salt thereof;
- wherein:
- stereochemical configurations depicted at asterisk positions indicate absolute stereochemistry;
- Ra is hydrogen;
- or Ra taken together with Rj and the intervening atoms forms a cyclic diol protecting group;
- Rb is hydrogen;
- Rc is hydrogen;
- Rd is hydrogen;
- Re is hydrogen;
- Re′ is hydrogen;
- each Rf is independently hydrogen;
- Rg′ is chloro, bromo, fluoro, or iodo;
- Rh is hydrogen;
- Rh′ is hydrogen;
- Rj is hydrogen;
- or Rj taken together with Ra and the intervening atoms forms a cyclic diol protecting group;
- Rk is hydrogen.
14 more elements
Dependencies are inferred from the claim text.