Method for preparing ivosidenib and an intermediate thereof

Inventors

SIZEMORE, JACOB PAUL • Zhang, Shijie • Vo, Nha Huu

Assignees

Servier Pharmaceuticals LLC

Abstract

The present application relates to a method for preparing a substantially and diastereomerically pure crystalline ethanol solvate of Compound IIa and its use for synthesizing Ivosidenib.

Core Innovation

The invention describes a crystalline ethanol solvate of Compound IIa and methods that prepare the solvate and use it in preparing Compound I. The supplied summary identifies dynamic crystallization of a Compound IIa/IIb diastereomer mixture, with selective crystallization of Compound IIa. It also states that the solvate is converted to Compound I, identified in the provided text as ivosidenib.

The supplied partial content characterizes the solvate through XRPD, DSC, TGA, and chemical or diastereomeric purity limitations in the claims. It also reports example results for isolated material, but those results do not establish a stated advantage in the provided text. The background section is absent from the supplied content, so the problem being solved is not explicitly described in patent.

Claims Coverage

The patent provides three inventive features across three independent claims, comprising two method claims and one composition of matter claim.

The independent claims cover preparation of Compound I through the crystalline ethanol solvate, preparation of that solvate, and the solvate as a product. Dependent claims further define the solvate by diffraction and purity characteristics.

Stated Advantages

Documented Applications