US 12,709,595 B2Granted

Synthetic pathway to belzutifan

AssigneeMerck Sharp & Dohme Corp.

InventorsDaniel A. DiRocco, Jackson Kenai Blender Cahn, Wai Ling Cheung-Lee, Stephanie W. Chun, J. Caleb Hethcox, Heather Claire Johnson, Jungchul Kim, Joshua N. Kolev, Birgit Kosjek, Diane Le, Scott D. McCann, John McIntosh, Jonathan P. McMullen, Jeffrey C. Moore, William Morris, Juan Esteban Velasquez Velez, Matthew S. Winston, Victoria Zhang, Yong-Li Zhong

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Abstract

The disclosure provides a novel process and synthetic intermediates for making belzutifan, a HIF-2α inhibitor, useful for the treatment of certain VHL-related indications and cancer.

Claims17

Dependent claims

A process for preparing belzutifan

comprising:
(a) contacting hydroxy indanone (5)
with a fluorinating agent under acidic conditions to yield fluoro hydroxyindanone (6),
(b) contacting the fluoro hydroxyindanone (6) with a ketoreductase comprising the full-length sequence of SEQ ID NO:2 to provide fluorodiol (7),
(c) isolating the fluorodiol (7), and
(d) converting fluorodiol (7) to belzutifan.

3 more elements

Dependencies are inferred from the claim text.

Facts

Application: 18/346,315Filed 3 Jul 2023 · us provisional application
Priority: 8 Jul 2022
Published: US 2024/0010613 A111 Jan 2024
Granted: 18 Aug 2026
Term ends: Not estimatedThe source records don’t support an estimate.

Classification17 codes

C07C 317/14
Sulfones; Sulfoxides: having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
C07C 45/455
By condensation: with carboxylic acids or their derivatives
C07C 51/09
Preparation of carboxylic acids or their salts, halides or anhydrides: from carboxylic acid esters or lactones
C07C 253/30
Preparation of carboxylic acid nitriles: by reactions not involving the formation of cyano groups