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    • 45. 发明公开
    • ASYMMETRIC MICHAEL AND ALDOL ADDITION USING BIFUNCTIONAL CINCHONA-ALKALOID-BASED CATALYSTS
    • 不公平的MICHAEL- UND ALDOLADDITION UNTER VERWENDUNG BIFUNKELLELLER KATALYSATOREN AUF CINCHONAALKALOIDBASIS
    • EP1758899A1
    • 2007-03-07
    • EP05758837.8
    • 2005-05-27
    • BRANDEIS UNIVERSITY
    • DENG, LiLI, Hongming
    • C07D453/04B01J31/02
    • C07D453/04B01J31/0237B01J31/0244C07B2200/07C07C205/45C07C205/51C07C205/53C07C205/55C07C205/56C07C231/18C07C253/30C07C281/02C07C315/04C07C2601/08C07C2601/14C07C2602/08C07C317/44C07C317/46C07C317/50C07C233/87C07C255/19C07C255/41
    • One aspect of the present invention relates to quinine-based and quinidine-based catalysts. Another aspect of the invention relates to a method of preparing a derivatized quinine-based or quinidine-based catalyst comprising 1) reacting quinine or quinidine with 5 base and a compound that has a suitable leaving group, and 2) converting the ring methoxy group to a hydroxy group. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral electron-deficient alkene or azo compound or prochiral aldehyde or prochiral ketone, comprising the step of: reacting a prochiral electron-deficient alkene or azo compound or prochiral aldehyde or prochiral 10 ketone with a nucleophile in the presence of a catalyst; thereby producing a chiral, non racemic compound; wherein said catalyst is a derivatized quinine or quinidine. Another aspect of the present invention relates to a method of kinetic resolution, comprising the step of reacting racemic chiral alkene with a nucleophile in the presence of a derivatized quinine or quinidine.
    • 本发明的一个方面涉及基于奎宁和奎尼丁的催化剂。 本发明的另一方面涉及一种制备衍生的基于奎宁或奎尼丁的催化剂的方法,其包括:1)将奎宁或奎尼丁与碱和具有合适离去基团的化合物反应,和2)将环甲氧基转化为 羟基。 本发明的另一方面涉及从前手电子缺乏烯烃或偶氮化合物或前手性醛或前手性酮制备手性,非外消旋化合物的方法,其包括以下步骤:使前手电子缺乏烯烃或偶氮 化合物或前手性醛或前手性酮与亲核试剂在催化剂存在下反应; 从而产生手性,非外消旋化合物; 其中所述催化剂是衍生的奎宁或奎尼丁。 本发明的另一方面涉及一种动力学拆分方法,其包括以下步骤:在衍生的奎宁或奎尼丁存在下使外消旋手性烯与亲核试剂反应。
    • 49. 发明公开
    • INCREASING THE HDL LEVEL AND THE HDL/LDL RATIO IN HUMAN SERUM BY BALANCING SATURATED AND POLYUNSATURATED DIETARY FATTY ACIDS
    • 增加HDL镜子和HDL / LDL比率人血清中的平衡组合饱和与多不饱和脂肪酸的饮食
    • EP0820307A1
    • 1998-01-28
    • EP96911560.0
    • 1996-04-02
    • BRANDEIS UNIVERSITY
    • SUNDRAM, KalyanaPERLMAN, DanielHAYES, Kenneth, C.
    • A21D2A21D13A23C19A23D9A23L1A61K31
    • A23D9/00A21D2/145A21D13/80A23C19/093A23L27/60A23L33/12A61K31/23A61K31/231A61K31/232
    • A method of increasing the HDL concentration and the HDL/LDL concentration ratio in human serum by providing a balance between a sufficient and required proportion of cholesterol-free saturated fatty acids in the daily dietary fat of the human and a sufficient and required, but not excessive, proportion of polyunsaturated fatty acids comprising linoleic acid in dietary fat, while the remaining proportion of fatty acids and energy from the dietary fat is provided by monounsaturated fatty acids comprising oleic acid. The saturated fatty acids must constitute between 20 % and 40 % by weight of the daily dietary fat based upon dietary fat accounting for 30 % of the total dietary energy consumption, and linoelic acid must constitute between 15 % and 40 % by weight of dietary fat. In this way, the required proportional intake of polyunsaturated fatty acids enhances the formation of HDL from VLDL and/or decreases the clearance of HDL, while an excessive proportional intake of polyunsaturated fatty acids and monounsaturated fatty acids is avoided to assure a sufficient dietary availability of saturated fatty acids which are required for sufficient VLDL synthesis and HDL production.
    • 增加HDL浓度,并通过在人的每日饮食中的脂肪和足够提供不含胆固醇的饱和脂肪酸的充足和所需比例之间的平衡人血清中HDL / LDL浓度比的方法和必需的,但不 的多不饱和脂肪酸,包括在膳食脂肪亚油酸,而脂肪酸和能量从膳食脂肪的剩余比例由单不饱和脂肪酸包括油酸提供过多,比例。 饱和脂肪酸必须按重量计基于膳食脂肪占总食物能量消耗的30%的日常饮食中的脂肪20%和40%之间构成,和亚油酸必须按重量计的饮食中的脂肪组成15和%之间%40 , 以这种方式,所需的比例摄取的多不饱和脂肪酸,从VLDL增强HDL的形成和/或降低HDL的间隙,而在过大的比例摄取的多不饱和脂肪酸和单不饱和脂肪酸被避免,以确保有足够的膳食可用性 饱和脂肪酸是必需的哪个足够VLDL合成和HDL生产。