会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明申请
    • PROCESS FOR PREPARATION OF 7-DEHYDROCHOLESTEROL
    • 制备7-脱氢胆甾醇的方法
    • WO2015170341A1
    • 2015-11-12
    • PCT/IN2015/000198
    • 2015-05-06
    • FERMENTA BIOTECH LIMITED
    • DATLA, AnupamaTAMORE, JagdishTRIVIKRAM, Sreenath
    • C07J9/00C07J31/00
    • C07J9/00C07J31/003
    • The invention discloses an improved cost-effective process for preparation of 7-Dehydrocholesterol of formula I with good yield and purity, comprising:a) epimerizing 7(alpha+beta) bromo protected cholesterol in presence of tetrabutyl ammonium bromide in toluene or a ketonic solvent or combinations thereof to obtain predominantly 7.alpha-bromo 3-protected cholesterol; b) Reacting 7.apha-bromo 3- protected cholesterol with substituted or unsubstituted thiophenol or its salts in presence of a liquor ammonia to obtain predominantly 7.beta.-thiophenyl)-3-protected cholesterol; c) Oxidizing 7. beta. - thiophenyl 3-protected cholesterol in presence of Cumene hydrogen peroxide and Titanium tetraisopropoxide to obtain 7. beta. -phenyl sulfoxide 3-protected cholesterol; d) Converting 7. beta. -phenyl sulfoxide 3-protected cholesterol into 7-Dehydro 3-protected cholesterol in presence of base; e) purifying 7-Dehydro 3-protected cholesterol by suspending in a suitable organic solvent; and f) Deprotecting the 7-Dehydro 3-protected cholesterol by treating with alkali in presence of methanol to obtain 7-Dehydrocholesterol followed by purification of 7-Dehydrocholesterol from an organic solvent.
    • 本发明公开了一种用于制备具有良好产率和纯度的式I的7-脱氢胆固醇的改进的成本有效的方法,其包括:a)在甲苯或酮溶剂中存在四丁基溴化铵的7(α+β)溴保护的胆固醇差向异构化 或其组合以主要获得7.α-溴3-保护的胆固醇; b)在液氨的存在下,将7-溴-3-保护的胆固醇与取代或未取代的苯硫酚或其盐反应,主要得到7.β-噻吩基)-3-保护的胆固醇; c)氧化7.β。 在苯甲酸过氧化氢和四异丙氧基钛的存在下,将噻吩-3-保护的胆固醇得到7.β。 苯基亚砜3-保护胆固醇; d)转换7. beta。 苯基亚砜将3-保护的胆固醇转化为7-脱氢3-保护的胆固醇,在碱的存在下; e)通过悬浮在合适的有机溶剂中纯化7-脱氢3-保护的胆固醇; 和f)通过在甲醇存在下用碱处理来脱保护7-脱氢3-保护的胆固醇,得到7-脱氢胆固醇,然后从有机溶剂中纯化7-脱氢胆固醇。