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Fused ring pyrimidine compound salt and crystal form, and preparation method and application thereof
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A technology for fused-ring pyrimidines and compounds, which is applied to salts, crystal forms of fused-ring pyrimidine compounds and their preparation and application fields, can solve the problems of low dissolution rate, easy moisture absorption, low absorption rate and the like
Active Publication Date: 2019-12-10
SHANGHAI MAXINOVEL PHARMA CO LTD +1
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[0005]
The technical problem to be solved by the present invention is to overcome the defects of low drugsolubility, easy hygroscopicity, low absorption rate, low stability and low dissolution rate of fused ring pyrimidine compounds in the prior art in the process of preparing drugs, thereby providing A salt, crystal form, preparation method and application of a fused-ring pyrimidine compound represented by formula 1
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Embodiment 1
[0117] Embodiment 1 The preparation of the fumarate of the condensed ring pyrimidine compound shown in formula 2
[0118] Weigh the compound N-[7-(4-fluoro-2-methoxyphenyl)-6-methylthieno[3,2-d]pyrimidin-2-yl]-1-(piperidine-4- base)-1H-pyrazol-4-amine (synthesized according to Patent CN106366093A Example 31) 100mg (0.228mmol, 1eq) into the vial, add 10mL 88% acetone-water solution, add the vial at about 50°C and stir until dissolved clear. 1.1mL ethanol solution (0.275mmol, 1.2eq) of fumaric acid with a concentration of 0.25mol / L was slowly added dropwise to the free base solution of fused ring pyrimidines, and stirred and reacted at 50°C for 1 hour, and then the solution was Slowly cool down to room temperature at a rate of 5°C / h, collect the solid and dry under vacuum at 40°C overnight.
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Abstract
The invention discloses a fused ring pyrimidine compound salt and crystal form, and a preparation method and an application thereof. A fused ring pyrimidine compound is N-[7-(4-fluoro-2-methoxyphenyl)-6-methylthieno[3,2-d]pyrimidin-2-yl]-1-(piperidin-4-yl)-1H-pyrazole-4-amine, and has the structure represented by the formula 1. The preparation method of the fused ring pyrimidine compound salt andcrystal form is simple; the fused ring pyrimidine compound salt and the crystal form of the fused ring pyrimidine compound salt at least have good stability, do not easily absorb moisture, have polymorphic forms, chemical stability and pharmacokinetics, and have improved solubility characteristics.
Description
technical field [0001] The invention relates to a salt, a crystal form, a preparation method and an application of a condensed ring pyrimidine compound. Background technique [0002] JAK-STAT (Janus kinase-signaltransducer and activator oftranscription) signaling pathway is a signal transduction pathway stimulated by cytokines, involved in many important biological processes such as cell proliferation, differentiation, apoptosis and immune regulation (Aaronson, D.S. et al. Science 2002, 296, 1653-1655; O'Shea, J.J. et al. Nat. Rev. Drug Discovery 2004, 3, 555-564). It widely exists in various tissue cells in the body, especially plays an important role in the differentiation, proliferation, and anti-infection of lymphoid cell lines, and participates in the interaction and signal transduction of various inflammatory factors (Kiesseleva T. et al. J. Gene, 2002, 285, 1-24). Tumor occurrence, growth, invasion and metastasis are related to JAK-STAT signal transduction pathway....
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