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US 2018/0022757 A1Published application
Synthesis of polycyclic-carbamoylpyridone compounds
AssigneeGilead Sciences, Inc.
InventorsAnna Chiu, John Enquist, JR., Nolan Griggs, Christopher Hale, Norihiro Ikemoto, Katie Ann Keaton, Matt Kraft, Scott E. Lazerwith, Michel Leeman, Zhihui Peng, Kate Schrier, Jonathan Trinidad, Jochem Van Herpt, Andrew W. Waltman
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Abstract
Methods of making compounds of Formula I are disclosed:
Claims20
1-123. (canceled)
A process to prepare a compound of Formula B-1•J-1 according to the following scheme:
- wherein the process comprises reacting the free acid of B-1 with about one to five equivalents of J-1;
- and
- wherein
- Hal is halogen,
- n is 1, 2, or 3, and
- Ra is (C1-C4)alkyl, (C6-C10)aryl, or (C6-C10)aryl (C1-C4)alkyl.
3 more elements
133-145. (canceled)
A process for preparing a salt of formula B-1•J-1
- wherein the process comprises dissolving the free acid of B-1 and adding one equivalent of J-1,
- wherein
- Hal is halogen,
- n is 1, 2, or 3,
- Ra is (C1-C4)alkyl, (C6-C10)aryl, or (C6-C10)aryl(C1-C4)alkyl.
2 more elements
147-152. (canceled)
A compound having the following structure:
154-193. (canceled)
A process to prepare a compound of formula C-1
- wherein the process comprises reacting a compound of formula B1•J-1 with about 0.1 to 1 equivalent of a suitable acid, and
- wherein
- Hal is halogen, which may be the same or different,
- n is 1, 2, or 3, and
- Ra is (C1-C4)alkyl, (C6-C10)aryl, or (C6-C10)aryl(C1-C4)alkyl.
2 more elements
198-242. (canceled)
Dependencies are inferred from the claim text.