A crystal form of baricitinib and preparation method thereof
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A baricitinib and crystal form technology, applied in the field of baricitinib crystal form A and its preparation, can solve the problem of unfavorable crystal form conversion, instability of baricitinib, and strong hygroscopicity easily occurring, etc. problem, to achieve the effect of excellent high temperature stability and good bioavailability
Inactive Publication Date: 2018-08-10
SHANGHAI SUNTRONG BIOTECH
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Problems solved by technology
[0009] The problem to be solved by the present invention is to solve the existing baricitinib instability, strong hygroscopicity and easy crystal transformation, etc., which are unfavorable for its use in pharmaceutical processing and pharmaceutical compositions. The new crystal form of baricitinib provides more qualitative and quantitative information for the efficacy research of its solid drug
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Embodiment 1 to 6
[0035] Embodiments 1 to 6 Preparation of Baricitinib A Crystal Form
[0036] Weigh 800 mg of baricitinib raw material into a container, add 1.5 mL of N,N dimethylformamide to completely dissolve it. Slowly add 50 mL of the solvent in Table 1 (analytical grade, water is deionized water) to the obtained solution respectively, let it stand overnight, filter, and vacuum-dry to obtain an off-white solid. Weigh and calculate its yield, and the results are shown in Table 1.
[0037] Table 1 Preparation of baricitinib A crystal form
[0038] Example
Embodiment 7 to 12
[0039] Examples 7 to 12 Preparation of crystal form A of baricitinib
[0040] Weigh 1.0 g of baricitinib raw material into a container, add 1.0 mL of N,N dimethylformamide to completely dissolve it. Slowly add 60 mL of the solvent in Table 1 (analytical grade, water is deionized water) to the obtained solution respectively, let it stand overnight, filter, and vacuum-dry to obtain an off-white solid.
Embodiment 13 to 18
[0041] Examples 13 to 18 Preparation of crystal form A of baricitinib
[0042]Weigh 100mg of baricitinib raw material into a container, add 0.5mL N,N dimethylformamide to dissolve it completely. Slowly add 10 mL of the solvent in Table 1 (analytical grade, water is deionized water) to the obtained solution respectively, let it stand overnight, filter, and vacuum-dry to obtain an off-white solid.
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Abstract
The invention provides an A crystal form of baricitinib. Positions where 2-theta equals to 12.46, 13.921, 14.94, 15.359, 16.26, 16.639, 17.36, 19.08, 20.321, 21.961, 22.381, 24.118, 25.42, 27.441, 28.381, 29.321, 29.799, 32.675, 33.14, 33.563, 33.923 and 41.6 have diffraction peaks, wherein the error range of the 2-theta value is + / - 0.2. The provided A crystal form of the baricitinib has good high-temperature stability, high-humidity stability and illumination stability, can be applied to the medicine treating or preventing diseases related to JAK, has better bioavailability, and provided qualitative and quantitative information has very important significance for further studying the curative effect of the solid drugs.
Description
technical field [0001] The present invention relates to a polymorphic form of baricitinib as a JAK inhibitor, in particular to a polymorphic form of baricitinib A and a preparation method thereof. Background technique [0002] JAK, Janus Kinase, is a non-receptor tyrosine protein kinase and a non-transmembrane tyrosine kinase. This is because JAK can not only phosphorylate the cytokine receptors associated with it, but also phosphorylate multiple signaling molecules containing specific SH2 domains. The JAK protein family consists of four members: JAK1, JAK2, JAK3 and TYK2, which have seven JAK homology domains (JAK homology domain, JH) in structure, of which the JH1 domain is the kinase domain and the JH2 domain is the " The "pseudo" kinase domain, JH6 and JH7, are receptor binding regions. [0003] TYK2 is a potential target for immunoinflammatory diseases, which has been confirmed by human genetics and mouse knockout studies (Levy D. and Loomis C., New England Journal of...
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