Abacavir crystal and preparation method thereof

A crystal and X-ray technology, applied in the field of medicinal chemistry, can solve the problems that are not suitable for industrial production and large-scale preparation of preparations, and achieve the effects of easy operation and large-scale, high purity and stable form
CN105315280AInactive Publication Date: 2016-02-10SHANGHAI DESANO CHEM PHARMA +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI DESANO CHEM PHARMA
Publication Date
2016-02-10
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an abacavir crystal and a preparation method thereof. Under powder X-ray diffraction, the crystal has main characteristic peaks at the diffraction angle 2[theta] of 9.0 degrees, 10.1 degrees, 12.7 degrees, 13.2 degrees, 17.8 degrees, 20.2 degrees, 23.8 degrees and 25.5 degrees, wherein test error is + / - 0.2 degrees. The preparation method comprises the following steps: adding an abacavir raw material to an organic solvent, increasing the temperature until the solution is clear, dropwisely adding an anti-solvent at 50-60 DEG C, and then performing temperature-maintained stirring for 1-2 h, finally reducing the temperature to room temperature, collecting the separated-out crystal and drying the crystal. The abacavir crystal has stable form, is easy to separate, is high in purity and is stable in quality. The preparation method is simple in process, is easy to operate and achieve in large scale, and is beneficial to development and large-scale production of a follow-up preparation.
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Description

technical field

[0001] The invention relates to an abacavir crystal and a preparation method thereof, belonging to the technical field of medicinal chemistry. Background technique

[0002] Abacavir is an antiretroviral drug launched by GlaxoSmithKline. It is a carbocyclic 2'-deoxyguanosine drug, which is an inactive precursor like other nucleoside reverse transcriptase inhibitors medicine. Its chemical structure is shown below:

[0003]

[0004] At present, reports on the forms of abacavir mainly include: anhydrous, amorphous and acetone, ethyl acetate solvate. Some literatures describe methods for isolating abacavir by grinding or chromatography, but the result is always a gum-like solid or solid foam, which is difficult to achieve industrial scale operation.

[0005] WO9852949 describes the preparation of abacavir from acetone, during the preparation of abacavir free base an amorphous solid is produced which absorbs the solvent and is therefore not suitable for use w...

Claims

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