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PRODUCTION METHOD FOR ULIPRISTAL ACETATE AND ITS INTERMEDIATES
专利权人:
UTOPHARM (SHANGHAI) CO.; LTD
发明人:
LUO Junzhi (CN),ЛУО Янцзы (CN),SUN Yongqiang (CN),САН Йонциан (CN),LUO Xun (CN),ЛУО Сянь (CN),YAN Yimin (CN),ЯНЬ Иминь (CN),WANG Zhaojun (CN),ВАН Чжаоджан (CN),QIAN Mingxia (CN),ЦИАНЬ Минся (CN),TU Yo,LUO Junzhi,ЛУО Янцзы,SUN Yongqiang,САН Йонциан,LUO Xun,ЛУО Сянь,YAN Yimin,ЯНЬ Иминь,WANG Zhaojun,ВАН Чжаоджан,QIAN Mingxia,ЦИАНЬ Минся,TU Yongrui,ТУ Йонруи
申请号:
RU2014120908
公开号:
RU0002624007C2
申请日:
2012.07.12
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: biotechnology.SUBSTANCE: invention relates to a method of producing ulipristal acetate which includes the following stages:where R is a hydroxyl protective group isolated from -CH(CH3)-OR1, where R1 is isolated from C1-C10 of alkyl and the dashed lines in formula V represent the double bonds in 5(10), 9(11) or 4(5), 9(10). The method also comprises of the following stages: a) use of 3.3-(ethylene dioxyl)-19-norpregn-5(10), 9(11)-diene-3.17-dione by formula II as the starting material and the use of spirits as the reaction solvent with cyan reagent to prepare the compound 3.3-(ethylene dioxy)-17β-cyano-7α-hydroxyl-19-norpregn-5(10), 9(11)-diene by formula III in a faintly acid medium at a temperature from -10°C to the room temperature; b) the production of the compound by formula IV via the reaction of the compound by formula III and hydroxyl protective group of the reagent in an acid medium in a solvent; c) interaction of the compound by formula IV with a methylating reagent and hydrolysis of compound by formula IV in an acid medium after a methylating reaction to obtain 5(10), 9(11)-diene-3.20-dione or 4(5), 9(10)-dienen-3.20-dione by formula V, or their mixture; d) interaction of the compound by formula V with ethylene glycol by the catalysis of p- toluenesulfonic acid and trimethyl orthoformate or triethyle orthoformate at the room temperature in dichloromethane with the yield of the compound 3.3-(ethylene-dioxy)-17α-hydroxy-19-norpregn-5(10), 9(11)-diene by formula VI; e) epoxidation of the compound in formula VI by hydrogen peroxide with the yield of the compound 3,3,20,20-bis (ethylene dioxyl)-17α-hydroxyl-5,10-epoxy-19-norpregn-9(11)-en by formula VII; f) additional reaction between the compound by formula VII and 4-(N, N-dimethyl amidogen) phenyl magnesium bromide of the Grignard reagent with the yield of the compound 3,3,20,20-bis(ethylene dioxy)-5α-17α-dihydroxy-11β--[4-(N,N-dimethylamino)-phenyl-]-19-norpregn-9(11)-en by formula VIII; g) the hydrol
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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