Selective estrogen receptor degraders
AssigneeEli Lilly and Company
InventorsJolie Anne Bastian, Jeffrey Daniel Cohen, Almudena Rubio, Daniel Jon Sall, Jennifer Anne Mcmahon
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Abstract
Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, and the other is hydrogen, and methods for their use are provided.
Claims12
A process for preparing a compound of the formula
- the process comprising:
- treating a racemic compound of the formula
- with a base, in a solvent, wherein the base comprises sodium hydride and the solvent comprises tetrahydrofuran.
A process for preparing (4-{2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy}phenyl){3-[2-fluoro-4-(trifluoromethyl)phenyl]-7-hydroxyquinolin-4-yl}methanone Isomer 1, the process comprising reducing
- with a chiral reducing agent in a solvent, wherein the chiral reducing agent is made by treating (R)-(+)-α.α-diphenyl-2-pyrrolidinemethanol with trimethylborate and the solvent is tetrahydrofuran.
A process for preparing enantioenriched, isomer 1 of compound of the formula
- the process comprising treating (4-{2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy}phenyl)(hydroxy)methyl]-3-[2-fluoro-4-(trifluoromethyl)phenyl]quinolin-7-ol, isomer 1, with a base in a solvent, wherein the base comprises cesium carbonate and the solvent comprises dimethylsulfoxide.
Dependencies are inferred from the claim text.