Siponimod crystal form and preparation method thereof

A crystal form and X-ray technology, applied in the field of siponimod crystal form and its preparation, can solve the problems of poor stability or solubility of siponimod free base
CN110776450AActive Publication Date: 2020-02-11SUNSHINE LAKE PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SUNSHINE LAKE PHARM CO LTD
Publication Date
2020-02-11

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Abstract

The invention provides a siponimod crystal form and a preparation method thereof, and belongs to the field of medicinal chemistry, wherein the crystal form has good solubility and good stability. Thepreparation method comprises: mixing siponimod and a solvent, optionally adding an anti-solvent, stirring, and filtering to obtain the siponimod crystal form. According to the invention, the preparation method is simple to operate, mild in condition and beneficial to implementation in production.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry, in particular, the invention relates to a siponimod crystal form and a preparation method thereof. Background technique

[0002] BAF-312 (SiponiMod) Siponimod is a second-generation S1P receptor modulator that selectively acts on S1P1 and S1P5 receptors, and is more selective than S1P2, S1P3 and S1P4 receptors. Studies have shown that siponimod can effectively delay the progression of disability in secondary multiple sclerosis.

[0003] The structure of siponimod is shown in formula (I):

[0004]

[0005] At present, there have been reports disclosing the crystal form A of siponimod free base and providing solubility data, but the solubility of crystal form A is average.

[0006] The crystal form of a drug is an important factor affecting the quality of a drug. Different crystal forms of the same drug molecule will have significant differences in appearance, solubility, melting point, diss...

Claims

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