SYNTHESIS OF FATTY ALCOHOL ESTERS OF α-HYDROXY CARBOXYLIC ACIDS AND THEIR USE AS PERCUTANEOUS ABSORPTION ENHANCERS
    4.
    发明申请
    SYNTHESIS OF FATTY ALCOHOL ESTERS OF α-HYDROXY CARBOXYLIC ACIDS AND THEIR USE AS PERCUTANEOUS ABSORPTION ENHANCERS 审中-公开
    α-羟基羧酸的脂肪醇酯的合成及其作为渗透吸收增强剂的使用

    公开(公告)号:WO2006044926A2

    公开(公告)日:2006-04-27

    申请号:PCT/US2005/037504

    申请日:2005-10-17

    Abstract: The present invention provides a novel approach for the preparation of fatty alcohol esters of α-hydroxy carboxylic acids. In one form of the invention, the target fatty alcohol ester of α-hydroxy carboxylic acid is produced by converting a lower alkyl ester of α-hydroxy carboxylic acid into a fatty alcohol ester of α-hydroxy carboxylic acid via alcoholysis (i.e., transesterification). The transesterification process is an equilibrium reaction, catalyzed chemically (i.e., with acids or bases) or enzymatically, that is shifted in the desired direction to produce the desired product. One preferred way of shifting the reaction in the direction of the desired product is by reducing the concentration of one of the products (e.g., distillation of a lower-boiling alcohol as soon as it is formed). Another preferred way of shifting the reaction in the direction of the desired product is by increasing the concentration of one of the reactants (e.g., adding more of the starting ester).

    Abstract translation: 本发明提供了一种制备α-羟基羧酸的脂肪醇酯的新方法。 在本发明的一种形式中,α-羟基羧酸的目标脂肪醇酯通过醇解(即酯交换)将α-羟基羧酸的低级烷基酯转化为α-羟基羧酸的脂肪醇酯而产生, 。 酯交换方法是平衡反应,在化学上(即酸或碱)或酶促催化,其在所需方向上移动以产生所需产物。 在所需产物的方向上移动反应的一种优选方法是通过降低其中一种产物的浓度(例如,一旦形成低沸点醇即可蒸馏)。 在所需产物的方向上移动反应的另一种优选方法是通过增加一种反应物的浓度(例如,加入更多的起始酯)。

    SYNTHESIS OF (6S)-5-METHYL-5,6,7,8-TETRAHYDROFOLIC ACID
    5.
    发明申请
    SYNTHESIS OF (6S)-5-METHYL-5,6,7,8-TETRAHYDROFOLIC ACID 审中-公开
    (6S)-5-甲基-5,6,7,8-四氢叶酸的合成

    公开(公告)号:WO2007084738A2

    公开(公告)日:2007-07-26

    申请号:PCT/US2007/001574

    申请日:2007-01-22

    CPC classification number: C12P17/182 C07D475/04

    Abstract: A process for the large-scale chemoenzymatic production of (6S)-5-methyl-5,6,7,8-tetrahydrofolic acid, also known as (6S)-5-methylTHFA, the process comprising the steps of: (1) reducing folic acid (FA) so as to yield dihydrofolic acid (DHFA); (2) stereoselective reducing DHFA with dihydrofolate reductase (DHFR) in the presence of NADP/NADPH, glucose and GluDH so as to yield (6S)-THFA; (3) converting (6S)-THFA to (6S)-5-methylTHFA; and (4) isolating (6S)-5-methylTHFA.

    Abstract translation: (6S)-5-甲基-5,6,7,8-四氢叶酸的大规模化学酶生产方法,也称为(6S)-5-甲基THFA,方法 包括以下步骤:(1)减少叶酸(FA)以产生二氢叶酸(DHFA); (2)在NADP / NADPH,葡萄糖和GluDH存在下用二氢叶酸还原酶(DHFR)立体选择性还原DHFA以产生(6S)-THFA; (3)将(6S)-THFA转化成(6S)-5-甲基THFA; 和(4)分离(6S)-5-甲基THFA。

    COMPOSITIONS COMPRISING FOLIC ACID DERIVATIVES. THEIR PREPARATIONS AND METHODS OF USE
    7.
    发明申请
    COMPOSITIONS COMPRISING FOLIC ACID DERIVATIVES. THEIR PREPARATIONS AND METHODS OF USE 审中-公开
    包含叶酸衍生物的组合物。 他们的准备和使用方法

    公开(公告)号:WO2014018873A3

    公开(公告)日:2014-01-30

    申请号:PCT/US2013/052304

    申请日:2013-07-26

    Abstract: Described herein are nutritional compositions (e.g., oral dosage forms and vitamin supplements) of folic acid derivatives such as a compound of formula (V) and methods of making a compound of formula (V) by cyclization of 5-formyl-(6S)-tetrahydrofolate. Also provided are methods of making L-methylfolate by borohydride reduction of said intermediate compound of formula (V).

    Abstract translation: 本文描述了叶酸衍生物例如式(V)化合物的营养组合物(例如口服剂型和维生素补充剂)以及通过环化式(V)化合物制备式(V)化合物的方法 5-甲酰基 - (6S) - 四氢叶酸。 还提供了通过硼氢化物还原所述式(V)的中间体化合物来制备L-甲基叶酸的方法。

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