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Use of a pyrimidine derivative in the preparation of a drug for preventing and/or treating and/or adjuvantly treating tumors
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A pyrimidine derivative and adjuvant therapy technology, applied in the field of medicine, can solve problems such as time lag and arrhythmia
Active Publication Date: 2015-11-25
刘强 +1
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Studies have found that the drug can cause the patient's risk of QTc prolongation (QTc is the time difference between the corrected T wave and Q wave on the electrocardiogram, and QTc prolongation can easily lead to arrhythmia). In November 2007, Merck terminated the Phase II of VX-680 Clinical trials (ExpertOpin.InvestingDrugs.2009, 18, 379)
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Embodiment 1
[0081] Synthesis of compound B:
[0082] Weigh 2,4,6-trichloropyrimidine (1.83g, 10mmol), 3-amino-5-methylpyrazole (0.97g, 10mmol) dissolved in 100mL absolute ethanol, add 1.4mL triethylamine, 0 The reaction was stirred at ℃ for 12h. After stopping the reaction, 150 mL of water was added to the reaction solution, and a large amount of white solid precipitated out immediately, which was filtered by suction, washed with 50 mL of ice water and 20 mL of ice methanol, and dried to obtain white solid B (1.82 g, 75%).
[0083] Product analysis: the NMR data of the obtained white solid B is 1 HNMR (400MHz, DMSO-d 6 )δ: 12.21(s, 1H), 10.63(s, 1H), 7.74 and 6.76(m, 1H), 6.38, 5.78(m, 1H), 2.21(s, 3H); 13 CNMR (100MHz, DMSO-d 6 )δ: 161.1, 159.7, 158.4, 147.1, 139.0, 102.6, 95.2, 10.4ppm. It can be seen that the obtained white solid B has the structure in structural formula (2).
[0084] Synthetic Compound A:
[0085] Compound B (244mg, 1.0mmol), p-nitroaniline (166mg, 1.2mmol), an...
Embodiment 2
[0091] Synthesis of Compound B:
[0092] Weigh 2,4,6-trichloropyrimidine (1.83g, 10mmol), 3-amino-5-methylpyrazole (1.94g, 20mmol) dissolved in 100mL absolute ethanol, add 1.4mL triethylamine, 0 The reaction was stirred at ℃ for 16h. After stopping the reaction, 150 mL of water was added to the reaction solution, and a large amount of white solid precipitated immediately, which was filtered by suction, washed with 50 mL of ice water and 20 mL of ice methanol in turn, and dried to obtain white solid B (1.82 g, 70%).
[0093] Synthetic Compound A:
[0094]Compound B (244mg, 1.0mmol), p-nitroaniline (138mg, 1mmol), and p-toluenesulfonic acid monohydrate (190mg, 1mmol) were weighed, dissolved in 10mL of n-butanol, and refluxed at 150°C for 10h. After cooling to room temperature, 2.5 mL of saturated NaHCO was added 3 solution, neutralized to pH=7-8, extracted with dichloromethane (20mL×3), and the organic layer was washed with anhydrous Na 2 SO 4 After drying, the solvent was ...
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Abstract
The invention discloses application of a pyrimidine derivative in preparation of drugs capable of prevention and / or treatment and / or adjuvant therapy of tumors. The pyrimidine derivative comprises a pyrimidine compound having a structural formula (I), a pharmaceutically acceptable salt thereof, a solvate, a polymorphic substance, a tautomer and a prodrug or a composition containing the pyrimidine compound. The structural formula (I) is described in the specification. According to the invention, the novel pyrimidine derivative with Aurora kinase inhibition activity is formed through different C-N couplings and introduction of different pharmacophores respectively at positions 2, 4 and 6 of a pyrimidine ring, and the pyrimidine derivative can be used for preparation of drugs capable of prevention and / or treatment and / or adjuvant therapy of tumors.
Description
technical field [0001] The invention relates to the field of medicine, in particular to the use of a pyrimidine derivative in the preparation of drugs for preventing and / or treating and / or adjuvantly treating tumors. Background technique [0002] Aurora kinases are a class of serine / threonine kinases that play an important regulatory role in the cell growth cycle. They are involved in the regulation of spindle formation, centrosome maturation, chromosome differentiation and cytokinesis, and play a key role in maintaining genome stability. Studies have found that the overexpression of Aurora kinases can easily lead to abnormal cell mitosis, which is closely related to the formation of tumors. Aurora kinase is overexpressed in many cancer cells (such as lung cancer, breast cancer, rectal cancer, thyroid cancer, pancreatic cancer), and inhibiting the activity of Aurora kinase can lead to polyploid aggregation of tumor cells, promote cell apoptosis, and block cell proliferation ...
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