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    • 10. 发明公开
    • 구굴스테론의 제조방법
    • 生产防腐剂的方法
    • KR1020030033504A
    • 2003-05-01
    • KR1020010065507
    • 2001-10-23
    • 동방에프티엘 주식회사
    • 김영배이정권최선희강문석
    • C07J13/00
    • C07J13/007A61K31/56
    • PURPOSE: Provided are Z- and E-type guggulsterone, which inhibits subcutaneous fat and has anti-fatness and cholesterol inhibiting activities and are produced from 16-dihydro pregnaron acetate. CONSTITUTION: The Z- and E-type guggulsterone(formula 2a and 2b) having the ratio of 80:20 are produced by a process comprising the steps of: reducing the 16-dihydro pregnaron acetate in an organic solvent by Red-Aldrich to prepare 5,16-pregnadiene-3beta-20 diol, wherein the organic solvent is toluene, xylene, cumene, or methyl ethyl ketone; oxidizing the 5,16-pregnadiene-3beta-20 diol by p-toluene sulfonic acid to prepare a mixture of 5,17(20)-trans pregnadiene-3beta, 16beta and 3beta, 16alpha diacetate; dissolving the mixture of 5,17(20)-trans pregnadiene-3beta, 16beta and 3beta, 16alpha diacetate in methanol solution in which potassium hydroxide is dissolved and refluxing to obtain 5,17(20)-trans pregnadiene-3beta, 16beta and 3beta, 16alpha diol; oxidizing the 5,17(20)-trans pregnadiene-3beta, 16beta and 3beta, 16alpha diol by NiO in the presence of a hydrogen acceptor mixture of cyclopentanone and acetone.
    • 目的:提供Z型和E型古格斯酮,其抑制皮下脂肪并具有抗脂肪和胆固醇抑制活性,并由16-二氢孕烯乙酸酯制备。 构成:通过包括以下步骤的方法产生具有80:20比例的Z型和E型格格酮(式2a和2b),该方法包括:通过Red-Aldrich在有机溶剂中还原16-二氢孕烯乙酸酯以制备 5,16-孕二烯-3β-20二醇,其中有机溶剂是甲苯,二甲苯,异丙基苯或甲基乙基酮; 通过对甲苯磺酸氧化5,16-孕二烯-3β-20二醇以制备5,17(20) - 反式孕二烯-3β,16beta和3β,16α二乙酸酯的混合物; 将5,17(20) - 反式孕二烯-3βeta,16beta和3β,16α二乙酸酯的混合物溶解在其中溶解氢氧化钾并回流的甲醇溶液中,得到5,17(20) - 反式孕二烯-3βeta,16beta和3β ,16α二醇; 在环戊酮和丙酮的氢受体混合物存在下,通过NiO氧化5,17(20) - 反式孕二烯-3β,16beta和3β,16α二醇。