PRACTICAL AND EFFICIENT SYNTHETIC METHOD OF RETINOIC ACID AND ITS DERIVATIVES
    2.
    发明申请
    PRACTICAL AND EFFICIENT SYNTHETIC METHOD OF RETINOIC ACID AND ITS DERIVATIVES 审中-公开
    杀真菌及其衍生物的实用有效合成方法

    公开(公告)号:WO02044140A1

    公开(公告)日:2002-06-06

    申请号:PCT/KR2001/002078

    申请日:2001-12-01

    摘要: The present invention provides allylic disulfone of Chemical Formula 1, an important intermediate which can be used for syntheses of retinoids and carotenoids, a process for preparing the same, and a process for preparing retinoid compounds by using the said intermediate, and, in particular, a process for preparing retinoic acid of Chemical Formula 2 and alkyl retinoate of Chemical Formula 3. The process for preparing allylic disulfone compound of Chemical Formula 1 employs cyclo-geranyl sulfone, which reacts with C5 haloallylic sulfide to give rise to the chain-extended C15 thio-sulfone compound. The thio-sulfone compound is selectively oxidized to give allylic disulfone of Chemical Formula 1. The C15 disulfone compound reacts with C5 halo-acid or C5 halo-ester under the condition using excess base, which induces coupling and subsequent desulfonation reactions to give retinoic acid of Chemical Formula 2 or alkyl retinoate of Chemical Formula 3.

    摘要翻译: 本发明提供了化学式1的烯丙基二砜,其可用于合成类视色素和类胡萝卜素的重要中间体,其制备方法和通过使用所述中间体制备类视色素化合物的方法,特别是, 制备化学式2的视黄酸和化学式3的视黄酸的方法。化学式1的烯丙基二砜化合物的制备方法使用环芴基砜,其与C 5卤代硫代硫酸反应产生链延长的C15 硫代砜化合物。 硫代砜化合物被选择性氧化,得到化学式1的烯丙基二砜.C15二砜化合物在使用过量碱的条件下与C5卤代酸或C5卤代酯反应,引起偶联和随后的脱磺化反应,得到视黄酸 的化学式2或化学式3的视黄酸烷基酯。

    HIGH SURFACE MICROPOROUS MATERIALS WHICH ARE ACTIVE IN OXIDATION REACTIONS. TIQ-6 AND METIQ-6
    3.
    发明申请
    HIGH SURFACE MICROPOROUS MATERIALS WHICH ARE ACTIVE IN OXIDATION REACTIONS. TIQ-6 AND METIQ-6 审中-公开
    在氧化反应中活性高的高表面微孔材料。 TIQ-6和METIQ-6

    公开(公告)号:WO01037629A2

    公开(公告)日:2001-05-31

    申请号:PCT/ES2000/000456

    申请日:2000-11-24

    摘要: The invention relates to a microporous material formed by oxygen, silicon, germanium, aluminum, boron, gallium, zirconium and/or titanium known as TIQ-6, to a method for preparing said material and to its applications as catalyst in oxidation reactions. The TIQ-6 preparation method is based on the synthesis of a gel containing titanium and/or zirconium, hydrothermal treatment thereof under controlled conditions and treatment of the resulting laminar material with an organic compound solution, preferably having a long hydrocarbonated chain containing a proton accepting group. This swollen material is subjected to a specific treatment involving agitation, ultrasound or any other method known in prior art with the purpose of obtaining a delaminated solid with a high outer surface. The invention also relates to a material having similar characteristics as that of TIQ-6 but additionally having organic groups anchored on the surface thereof and called METIQ-6, to a method for preparing the latter and to the utilization thereof as catalyst in oxidation reactions. The incorporation of organic species during synthesis of the material called METIQ-6 is carried out by means of a post-synthesis process on the TIQ-6 material.

    摘要翻译: 本发明涉及一种由氧,硅,锗,铝,硼,镓,锆和/或钛称为TIQ-6形成的微孔材料,用于制备所述材料的方法及其在氧化反应中作为催化剂的应用。 TIQ-6制备方法是基于合成含有钛和/或锆的凝胶,在受控条件下进行水热处理,并用有机化合物溶液处理所得的层状材料,优选具有含有质子接受的长烃链 组。 该溶胀材料经受涉及搅拌,超声波或现有技术中已知的任何其它方法的具体处理,目的是获得具有高外表面的分层固体。 本发明还涉及具有与TIQ-6类似的特征的材料,但另外具有锚固在其表面上的称为METIQ-6的有机基团,其制备方法和用作氧化反应中的催化剂的方法。 在称为METIQ-6的材料的合成期间掺入有机物质是通过对TIQ-6材料的后合成方法进行的。

    SUBSTITUTED (E)-STYRYL BENZYLSULFONES FOR TREATING PROLIFERATIVE DISORDERS
    9.
    发明申请
    SUBSTITUTED (E)-STYRYL BENZYLSULFONES FOR TREATING PROLIFERATIVE DISORDERS 审中-公开
    用于治疗增殖性疾病的替代(E) - 氨苄青霉素

    公开(公告)号:WO02028828A1

    公开(公告)日:2002-04-11

    申请号:PCT/US2001/031337

    申请日:2001-10-05

    摘要: (E)-Styryl benzylsulfones useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: R1 is selected from the group consisting of halogen, C1-C6 alkoxy, nitro, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); and R2 and R3 are independently selected from the group consisting of halogen, C1-C6 alkoxy, C1-C6 alkyl, nitro, cyano, hydroxy, phosphonato, amino, sulfamyl, carboxy, acetoxy, and dimethylamino (C2-C6 alkoxy); provided: R1 may not be halogen when R2 and R3 are both halogen; R2 may not be 2-halogen when R3 is 4-halogen; or a pharmaceutically acceptable salt thereof; or formula II: whrein: R4 is selected from the group consisting of C1-C6 alkoxy, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); R6 is selected from the group consisting of nitro, hydrogen, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); and R7 is selected from the group consisting of halogen, C1-C6 alkoxy, C1-C6 alkyl, nitro, cyano, hydroxy, phosphonato, amino, sulfamyl, carboxy, acetoxy, dimethylamino (C2-C6 alkoxy) and trifluoromethyl; provided R5 and R6 may not be hydrogen in the same compound; or a pharmaceutically acceptable salt thereof.

    摘要翻译: (E)根据式I提供了可用作抗增殖剂的抗增生剂的酪氨酸苄基砜:其中:R 1选自卤素,C 1 -C 6烷氧基,硝基,膦酰基,氨基,亚磺酰基 ,羧基,乙酰氧基和二甲基氨基(C 2 -C 6烷氧基); R 2和R 3独立地选自卤素,C 1 -C 6烷氧基,C 1 -C 6烷基,硝基,氰基,羟基,膦酰基,氨基,氨基磺酰基,羧基,乙酰氧基和二甲基氨基(C 2 -C 6烷氧基)。 条件是:当R 2和R 3都是卤素时,R 1可以不是卤素; 当R3为4-卤素时,R2不为2-卤素; 或其药学上可接受的盐; 或者式II:其中R 4选自C 1 -C 6烷氧基,膦酰基,氨基,氨基磺酰基,羧基,乙酰氧基和二甲基氨基(C 2 -C 6烷氧基)。 R 6选自硝基,氢,膦酰基,氨基,氨基磺酰基,羧基,乙酰氧基和二甲基氨基(C 2 -C 6烷氧基); 氰基,羟基,膦酰基,氨基,氨基磺酰基,羧基,乙酰氧基,二甲基氨基(C 2 -C 6烷氧基)和三氟甲基; R 7选自卤素,C 1 -C 6烷氧基,C 1 -C 6烷基, 条件是R5和R6可能不是同一化合物中的氢; 或其药学上可接受的盐。