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Carbazole aminoalcohol compound and its preparation method and application against parasitic diseases
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An anti-parasite and compound technology, applied in the application field of anti-parasitic diseases, can solve the problems of high cost, allergic reaction, easy recurrence of surgery, etc.
Active Publication Date: 2021-06-01
STATION OF VIRUS PREVENTION & CONTROL CHINA DISEASES PREVENTION & CONTROL CENT +1
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[0006] In summary, there is still a lack of effective methods for preventing and treating tapeworms and trematode parasites in this area. Therefore, there is an urgent need in this area to develop compounds and methods for effectively treating tapeworms and trematode parasites.
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preparation example Construction
[0138] In the present invention, a preparation method of a compound of formula A comprises steps:
[0139]
[0140] (a) in an aprotic polar solvent, in the presence of a base, the substituted carbazole shown in formula I is reacted with epichlorohydrin to obtain a compound of formula II; and
[0141] (b) in a protic polar solvent, under Lewis acid catalysis, the formula II compound and HNR 1 R 2 Carry out the reaction, thereby obtain formula A compound;
[0142] In the above formulas, X, Y, R 1 and R 2 is defined as above.
[0143] In another preferred example, the method includes:
[0183] 3,6-Dichlorocarbazole (470mg, 2mmol) was dissolved in 20mL DMF, and potassiumhydroxide (135mg, 2.4mmol) was slowly added under ice-bath conditions, and stirred for 0.5-1 hour after the addition, until the potassium hydroxide was solid completely dissolved.
[0184] Then epichlorohydrin (2.4 mmol) was slowly added dropwise into the system, and reacted for 4-5 hours. After the reaction, add 30ml of water, extract with ethyl acetate (30ml×3), wash with saturated sodiumchloride solution (30ml×3), dry the organic layer with anhydroussodiumsulfate, filter, and recover the solvent from the filtrate under reduced pressure, the crude product Purified by column chromatography to obtain 293 mg of white solid, yield 50%.
[0186] Refer to Example 1 for the operation process, and replace 3,6-dichlorocarbazole with carbazole to obtain a white solid with a yield of 70%.
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Abstract
The invention provides a class of carbazole aminoalcohol compounds, a preparation method thereof and an application in anti-parasitic diseases. Specifically, the present invention provides a racemate and enantiomer of the compound represented by formula (A) or a pharmaceutically acceptable salt thereof, the compound has excellent anti-schistosome and anti-echinococcosis activities. The invention has reasonable design, wide sources of raw materials, simple and convenient preparation method, is suitable for practical use, and can be applied in the preparation of antiparasitic medicines.
Description
technical field [0001] The invention belongs to the field of medicine, and in particular relates to a novel carbazole aminoalcohol compound, its preparation method and its application in anti-parasitic diseases. Background technique [0002] Schistosomiasis is a zoonotic parasitic disease that seriously endangers human health and affects social and economic development. According to the statistics of the World Health Organization, schistosomiasis ranks first among water-borne diseases and is one of the diseases with the widest geographical distribution among all parasitic diseases. Endemic in tropical and subtropical regions, the disease is one of the major neglected diseases threatening populations in developing countries. At present, schistosomiasis is prevalent in 76 countries and regions around the world, with a population of about 779 million and about 207 million infected people. [0003] So far there is no effective anti-schistosomiasis vaccine, chemotherapy is the ...
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