US 12,234,210 B2
Synthesis of nirogacestat
Kristin Patterson, Stamford, CT (US); and Mark Hatcher, Stamford, CT (US)
Assigned to SPRINGWORKS THERAPEUTICS, INC., Stamford, CT (US)
Filed by SpringWorks Therapeutics, Inc., Stamford, CT (US)
Filed on Apr. 20, 2023, as Appl. No. 18/304,202.
Application 18/304,202 is a continuation of application No. PCT/US2022/075839, filed on Sep. 1, 2022.
Claims priority of provisional application 63/239,696, filed on Sep. 1, 2021.
Prior Publication US 2023/0312480 A1, Oct. 5, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 233/88 (2006.01); C07C 227/26 (2006.01); C07D 263/44 (2006.01)
CPC C07D 233/88 (2013.01) [C07C 227/26 (2013.01); C07D 263/44 (2013.01)] 4 Claims
 
1. A composition comprising 98.0% to 99.9% by weight of Compound 1 or a salt thereof prepared by a process comprising the steps of combining Compound 10

OG Complex Work Unit Chemistry
with Compound 11

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to form Compound 1, and optionally treating Compound 1 with an acid in a solvent to form a salt of Compound 1

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wherein the composition comprises at least one of:
(a) 0.7% to 0.01% by weight of Compound 2 having the formula

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof,
(b) 0.7% to 0.01% by weight of Compound 3 having the formula

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof, or
(c) 0.7% to 0.01% by weight of Compound 4 having the formula

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof.