Process of making a menin-MLL inhibitor

A convergent synthesis of Compound A using solid-state intermediates and telescoped steps addresses inefficiencies in existing methods, enabling high-yield, scalable production suitable for pharmaceutical manufacturing.

WO2025232874A1 Publication Date: 2025-11-13KURA ONCOLOGY INC
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Patent Information

Application Number
PCT/CN2025/093750
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-05-10
Filing Date
2025-05-09
Publication Date
2025-11-13

AI Technical Summary

Technical Problem

Existing synthesis methods for Compound A, a potent menin-KMT2A (MLL) inhibitor, are inefficient, require multiple isolations and protection/deprotection steps, produce racemic products, and involve low-yielding chromatographic separations, making them unsuitable for large-scale manufacturing.

Method used

A convergent synthesis process using solid-state intermediates that can be purified by precipitation or crystallization, with high atom economy and yields, involving telescoped steps and safe, commercially available reagents to produce Compound A and its pharmaceutically acceptable salts.

Benefits of technology

The process achieves high purity and efficiency suitable for industrial-scale drug manufacturing, overcoming the limitations of previous methods by reducing the number of isolations and using scalable purification techniques.

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Abstract

Described herein are methods of making the menin-MLL inhibitor (S) -4-methyl-5- ( (4- ( (2-(methylamino) -6- (2, 2, 2-trifluoroethyl) thieno [2, 3-d] pyrimidin-4-yl) amino) piperidin-1-yl) methyl) -1-(2- (4- (methylsulfonyl) piperazin-1-yl) propyl) -1H-indole-2-carbonitrile (Compound A) and pharmaceutically acceptable salts thereof.
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