US 11,926,634 B2
Processes for the preparation of selective estrogen receptor degraders
Alonso Jose Arguelles Delgado, Indianapolis, IN (US); Boris Arnoldovich Czeskis, Carmel, IN (US); Mai Khanh Nguyen Hawk, Indianapolis, IN (US); Douglas Patton Kjell, West Lafayette, IN (US); Yu Lu, Zionsville, IN (US); Nicholas Andrew Magnus, Indianapolis, IN (US); and David Michael Remick, Fishers, IN (US)
Assigned to Eli Lilly and Company, Indianapolis, IN (US)
Filed by Eli Lilly and Company, Indianapolis, IN (US)
Filed on Jan. 27, 2023, as Appl. No. 18/160,457.
Claims priority of provisional application 63/409,060, filed on Sep. 22, 2022.
Claims priority of provisional application 63/305,520, filed on Feb. 1, 2022.
Prior Publication US 2023/0242545 A1, Aug. 3, 2023
Int. Cl. C07D 491/052 (2006.01); B01J 23/44 (2006.01)
CPC C07D 491/052 (2013.01) [B01J 23/44 (2013.01)] 20 Claims
 
1. A process for preparing a compound of Formula A:

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof, wherein either R1 or R2 is independently Cl, F, —CF3, or —CH3, and the other is H; and R7 is H or PG, wherein the process comprises reacting a compound of structure 8:

OG Complex Work Unit Chemistry
or a salt thereof, wherein R7 is PG or H; wherein PG is an alcohol protecting group, in a solvent with an amine of structure 9

OG Complex Work Unit Chemistry
or a salt thereof, and a reducing agent.