US 12,304,938 B2
Processes and intermediates for preparing tirzepatide
Michael Eugene Kopach, Greenwood, IN (US); Rachel Nicole Richey, Indianapolis, IN (US); Mark Richard Berglund, Zionsville, IN (US); Kevin Dale Seibert, Carmel, IN (US); and Emily Suzanne Murzinski, Zionsville, IN (US)
Assigned to Eli Lilly and Company, Indianapolis, IN (US)
Filed by Eli Lilly and Company, Indianapolis, IN (US)
Filed on Aug. 15, 2024, as Appl. No. 18/806,394.
Application 18/806,394 is a continuation of application No. PCT/US2023/086530, filed on Dec. 29, 2023.
Claims priority of provisional application 63/477,734, filed on Dec. 29, 2022.
Prior Publication US 2024/0400636 A1, Dec. 5, 2024
Int. Cl. C07K 14/605 (2006.01); C07K 14/00 (2006.01)
CPC C07K 14/605 (2013.01) [C07K 14/001 (2013.01)] 5 Claims
 
1. A process of preparing a compound of formula (I):

OG Complex Work Unit Chemistry
wherein PG is a protecting group, the process comprising:
(a) contacting a compound of formula (Ia) and diisopropylethylamine

OG Complex Work Unit Chemistry
(b) contacting the product of step (a) with 2-(5-norbornene-2,3-dicarboximido)-1,1,3,3-tetramethyluronium tetrafluoroborates in DMF; and
(c) adding a compound of formula (Ib) to the mixture of (b),

OG Complex Work Unit Chemistry