US 12,247,012 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 Sep. 30, 2022, as Appl. No. 17/937,283.
Application 17/937,283 is a continuation of application No. 17/929,153, filed on Sep. 1, 2022, granted, now 12,110,277.
Claims priority of provisional application 63/239,696, filed on Sep. 1, 2021.
Prior Publication US 2023/0091415 A1, Mar. 23, 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)] 15 Claims
 
1. A process for preparing a composition comprising Compound 1 or a pharmaceutically acceptable salt thereof which is susceptible to oxidation that is substantially free of Compound 13

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comprising the steps of:
i) dissolving Compound 11 in a solvent,

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ii) reacting Compound 9

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with 1,1′-carbonyldiimidazole to form Compound 10,

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and iii) combining Compound 10 with Compound 11 to form a composition comprising Compound 1 or a pharmaceutically acceptable salt thereof, where Compound 1 has the formula

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