Preparation method of cardiovascular drug ketanserin tartrate
A technology of tartaric acid and ketanserin is applied in the directions of carboxylate preparation, organic chemistry and the like, and achieves the effects of high yield, simple process synthesis steps and improved bioavailability
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Embodiment example 1
[0016] In the 2000ml four-neck bottle equipped with mechanical stirring, reflux condenser and thermometer, add 10g ketanserin, 10g tartaric acid and 1000ml absolute ethanol, under stirring, be heated to 78 ℃, reaction time 8 hours. Cool and crystallize. A white solid was obtained by suction filtration, and dried to a constant weight of 13 g of white crystalline powder, with a calculated yield of 81%. mp: 187-189°C (dec.), the content reaches 99.1%.
Embodiment example 2
[0018] In the 1000ml four-neck bottle equipped with mechanical stirring, reflux condenser and thermometer, add 10g ketanserin, 10g tartaric acid and 400ml 95% ethanol; Under stirring, be heated to 80 ℃, reaction time 8 hours. Cool and crystallize. A white solid was obtained by suction filtration, and dried to a constant weight of 12.8 g of white crystalline powder, with a calculated yield of 80%. mp: 187-189°C (dec.), the content reaches 99.2%.
Embodiment example 3
[0020] In the 1000ml four-neck bottle equipped with mechanical stirring, reflux condenser and thermometer, add 10g ketanserin, 10g tartaric acid and 350ml 85% ethanol; Under stirring, be heated to 85 ℃, reaction time 6 hours. Cool and crystallize. A white solid was obtained by suction filtration, and dried to a constant weight of 12.0 g of white crystalline powder, with a calculated yield of 75%. mp: 187-189°C (dec.), the content reaches 99.3%.
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