Method of making carotenoids
    3.
    发明授权
    Method of making carotenoids 有权
    制备类胡萝卜素的方法

    公开(公告)号:US6150561A

    公开(公告)日:2000-11-21

    申请号:US148088

    申请日:1998-09-04

    摘要: A widely applicable process for the manufacture of carotenoids by a Wittig reaction comprises carrying out the Wittig reaction in a polar reaction medium in a manner such that neither the reactants nor the thus-manufactured carotenoid are significantly dissolved in the reaction medium. An especially suitable reaction medium is a polar, toxicologically harmless solvent which remains monophasic on the addition of water in an amount up to about 30 vol. % and which permits the triarylphosphine oxide which is formed to dissolve well. Lower alcohols and acetone, as sole solvents or as mixtures with one another and/or with water, are especially suitable as the polar reaction medium. This process permits the use of much more concentrated reaction mixtures, simplifies the regeneration of the solvent and generally the reaction procedure, and avoids toxicologically objectionable solvents such as halogenated hydrocarbons.

    摘要翻译: 用于通过Wittig反应制造类胡萝卜素的广泛应用的方法包括在极性反应介质中进行Wittig反应,使得反应物和由此制得的类胡萝卜素都不会明显地溶解在反应介质中。 特别合适的反应介质是极性,毒理学上无害的溶剂,其在加入至多约30体积的量时保持单相。 %,这使得形成的三芳基氧化膦容易溶解。 作为唯一溶剂或作为彼此和/或与水的混合物的低级醇和丙酮特别适合作为极性反应介质。 该方法允许使用更浓缩的反应混合物,简化了溶剂的再生和通常的反应过程,并避免了毒理学上令人反感的溶剂如卤代烃。

    Intermediates for the preparation of vitamin A and carotenoids and
process for their preparation
    4.
    发明授权
    Intermediates for the preparation of vitamin A and carotenoids and process for their preparation 失效
    用于制备维生素A和类胡萝卜素的中间体及其制备方法

    公开(公告)号:US5663459A

    公开(公告)日:1997-09-02

    申请号:US473226

    申请日:1995-06-07

    摘要: The present invention relates to novel intermediates for the preparation of vitamin A and carotenoids corresponding to the formula (II): ##STR1## in which A represents a hydrogen or an alkyl, alkenyl or alkoxy group containing 1 to 4 carbon atoms, and X represents a carbon atom, and to a process for their preparation and their use, and further relates to compounds for preparing intermediates of formula (II) corresponding to the formula (III): ##STR2## in which R represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkylcarbonyl, alkenylcarbonyl, alkoxyalkyl or alkoxyalkenyl group in which the alkyl groups have 1 to 10 carbon atoms and the alkenyl groups have 2 to 10 carbon atoms, each of said groups being linear or branched and each being substituted or unsubstituted.

    摘要翻译: 本发明涉及用于制备对应于式(II)的维生素A和类胡萝卜素的新型中间体:其中A表示氢或含有1至4个碳原子的烷基,烯基或烷氧基, 并且X表示碳原子,并涉及其制备方法及其应用,还涉及制备对应于式(III)的式(II)的中间体的化合物:其中R表示 氢原子,碳原子数1〜10的烷基,碳原子数2〜10的烯基,烷基,碳原子数1〜10的烷基羰基,链烯基羰基,烷氧基烷基或烷氧基烯基,烯基具有2〜 10个碳原子,所述基团各自为直链或支链的,各自为取代或未取代的。

    Preparation of polyenes
    6.
    发明授权
    Preparation of polyenes 失效
    多烯的制备

    公开(公告)号:US5276209A

    公开(公告)日:1994-01-04

    申请号:US914128

    申请日:1992-07-17

    摘要: An improved process for the preparation of polyenes by the Julia reaction comprises carrying out the allylation of the anion of an allyl aryl sulfone generated a strong base, and the elimination of arylsulfinic acid to form a double bond in the same inert polar solvent which is immiscible with water, preferably in a ketone of the formula IR.sup.1 --CO--R.sup.2 (I)where R.sup.1 and R.sup.2 are each straight-chain or branched alkyl of 2 to 4 carbons, or R.sup.1 and R.sup.2 together are tetramethylene or pentamethylene. The process is particularly important for the preparation of vitamin A derivatives. In the preparation of vitamin A aldehyde, for example, it is advantageous to use the same alkali metal alcoholate as strong base in both stages so that the conversion can be carried out as one-pot reaction.

    摘要翻译: 通过Julia反应制备多烯的改进方法包括进行产生强碱的烯丙基芳基砜的阴离子的烯丙基化,以及消除芳基亚磺酸在与不混溶的相同惰性极性溶剂中形成双键 其中R1和R2分别是2至4个碳的直链或支链烷基,或者R1和R2一起是四亚甲基或五亚甲基。 该方法对于制备维生素A衍生物尤为重要。 在维生素A醛的制备中,例如,在两个阶段中使用相同的碱金属醇盐作为强碱是有利的,因此转化可以作为一锅反应进行。

    (20R)-2a-Methyl-19,26,27-Trinor-Vitamin D Analogs
    10.
    发明申请
    (20R)-2a-Methyl-19,26,27-Trinor-Vitamin D Analogs 有权
    (20R)-2a-甲基-19,26,27-三维 - 维生素D类似物

    公开(公告)号:US20080300223A1

    公开(公告)日:2008-12-04

    申请号:US12171085

    申请日:2008-07-10

    CPC分类号: C07C401/00

    摘要: This invention discloses (20R)-2α-methyl-19,26,27-trinor-vitamin D analogs, and specifically (20R)-2α-methyl-19,26,27-trinor-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also shows very low activity in vivo on bone calcium mobilization and intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.

    摘要翻译: 本发明公开了(20R)-2α-甲基-19,26,27-三硝基维生素D类似物,特别是(20R)-2α-甲基-19,26,27-三硝基-1α,25-二羟基维生素D 3和药物 用它。 该化合物显示转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性,因此证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如 皱纹,皮肤松弛,皮肤干燥,皮脂分泌不足。 与天然激素1α,25-二羟基维生素D 3相比,该化合物在体内对钙钙动员和肠钙运输活性的活性也显示出非常低的活性,因此可用于治疗人类的自身免疫性疾病或炎症性疾病以及肾性骨营养不良。 该化合物也可用于治疗或预防肥胖症。