Urea derivative and medicinal application thereof
A technology of urea groups and compounds, applied in the field of medicinal chemistry, can solve problems such as adverse reactions, multiple and serious, etc., and achieve the effect of practical therapeutic activity
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Embodiment 1
[0047] N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine-2 -yl)-2-methoxyacetamide fumarate
[0048] N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine- 59.3 g (0.1 mol) of 2-yl)-2-methoxyacetamide and 11.7 (0.1 mol) g of fumaric acid were dissolved in 1500 ml of boiling ethanol. The hot solution was filtered through diatomaceous earth, then slowly cooled under gentle stirring, and stood for several hours at a temperature of 0-5°C to precipitate N-(4-((4-(3-(3-tert-butyl -1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridin-2-yl)-2-methoxyacetamide fumarate crystals, filtered off N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine-2 The crystals of -yl)-2-methoxyacetamide fumarate were washed with ethanol and dried under vacuum at 50°C to obtain 63.3 g of product.
Embodiment 2
[0050] N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine-2 -yl)-2-methoxyacetamide fumarate
[0051] N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridine- 50.1 g of 2-yl)-2-methoxyacetamide fumarate and 12.2 g of fumaric acid were stirred in 1200 ml of refluxing ethanol until all the solids were dissolved. Add activated carbon, filter the hot solution through diatomaceous earth, and cool down to room temperature while stirring. Standing for several hours in a temperature environment of 0-5°C, N-(4-((4-(3-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)urea is precipitated Base) naphthalene-1-yloxy)methyl)pyridin-2-yl)-2-methoxyacetamide fumarate crystals, N-(4-((4-(3-(3-tert-butyl Base-1-p-tolyl-1H-pyrazol-5-yl)ureido)naphthalene-1-yloxy)methyl)pyridin-2-yl)-2-methoxyacetamide fumarate crystals, with Washing with ethanol and drying under vacuum at 50°C yielded 52.7 g of product.
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