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US 12,552,808 B2Granted
Diol desymmetrization by nucleophilic aromatic substitution
AssigneeAmgen Inc.
InventorsMatthew G. Beaver, Joseph Michael Dennis, Peter Dornan, Steven Mennen, Jason S. Tedrow, Neil F. Langille, Carolyn Michelle Cohen, Andreas Rene Rotheli
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Abstract
Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound Y that can be used to prepare them where the variable R1 is as defined herein. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof, compound A2, and salts and solvates thereof, and compound A3 and salts and solvates thereof.
Claims25
A process for synthesizing compound Y, or a salt thereof:
- comprising:
- admixing compound (I), compound (II), a catalyst, and a base in a bi-phasic solvent system to form compound Y:
- wherein
- R1 is CO2C1-6alkyl, CO2H, CON(C1-6alkyl)2, CO2Ar1, CO2Bn, or CN;
- Lg is a leaving group;
- and
- Ar1 is C6-22aryl or a 5-12 membered heteroaryl comprising 1 to 3 ring heteroatoms selected from O, N, and S.
4 more elements
Dependencies are inferred from the claim text.