New erlotinib hydrochloride crystal form and preparation method thereof

A technology of erlotinib hydrochloride and crystal form, applied in the field of medicinal chemistry, can solve the problems of environmental hazards, unsuitable for industrial production, high price of trifluorotoluene, etc., and achieve the effects of low toxicity, good solubility and stable crystal form
CN103435559BActive Publication Date: 2015-05-13SHANDONG JINCHENG PHARMACEUTICAL GROUP CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANDONG JINCHENG PHARMACEUTICAL GROUP CO LTD
Publication Date
2015-05-13

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Abstract

The present invention relates to a new erlotinib hydrochloride crystal form and a preparation method thereof, wherein the 2theta characteristic peaks are positioned at 9.395+ / -0.2 DEG, 13.197+ / -0.2 DEG, 15.507+ / -0.2 DEG, 16.797+ / -0.2 DEG, 20.019+ / -0.2 DEG, 20.511+ / -0.2 DEG, 20.944+ / -0.2 DEG, 22.273+ / -0.2 DEG, 22.795+ / -0.2 DEG, 24.270+ / -0.2 DEG, and 24.969+ / -0.2 DEG in an x-ray powder diffraction pattern. The preparation method comprises: (1) adding erlotinib base to a solvent, and stirring until the erlotinib base is dissolved; (2) introducing dry HCl gas until no solid is precipitated, and stirring; (3) cooling under stirring to achieve a temperature of 0-10 DEG C; and (4) filtering and drying to obtain the product. According to the present invention, the crystal form is single, and stability is good; and the alcohol is adopted as a solvent, such that characteristics of low toxicity, simple method, high product purity and easy industrial production are provided.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry and relates to a new crystal form of erlotinib hydrochloride and a preparation method thereof. Background technique

[0002] Erlotinib hydrochloride, trade name: Tarceva, chemical name: 4-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)quinazoline-hydrochloride 4-amine. Erlotinib hydrochloride, first listed in the United States in 2004, is a reversible epidermal growth factor tyrosinase (EGFR) inhibitor for locally advanced and or metastatic non-small cell lung cancer. The structural formula is as follows:

[0003]

[0004] According to literature and related patent reports, erlotinib hydrochloride has various crystal forms, including amorphous form, A crystal form, B crystal form, E crystal form, M crystal form, N crystal form, and P crystal form. The physical and chemical properties of each crystal form are quite different. For example, compared with crystal form A, crystal form B is ther...

Claims

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