SYNTHESIS OF (-)-BETA-ELEMENE, (-)-BETA-ELEMENAL, (-)-BETA-ELEMENOL, (-)-BETA-ELEMENE FLUORIDE AND THEIR ANALOGUES, INTERMEDIATES AND COMPOSITION AND USES THEREOF
    1.
    发明申请
    SYNTHESIS OF (-)-BETA-ELEMENE, (-)-BETA-ELEMENAL, (-)-BETA-ELEMENOL, (-)-BETA-ELEMENE FLUORIDE AND THEIR ANALOGUES, INTERMEDIATES AND COMPOSITION AND USES THEREOF 审中-公开
    ( - ) - BETA-ELEMENE,( - ) - BETA-ELEMENOL,( - ) - BETA-ELEMENE氟化物及其类似物,中间体和组合物的合成及其用途

    公开(公告)号:WO2006016912A3

    公开(公告)日:2007-02-15

    申请号:PCT/US2005014699

    申请日:2005-05-02

    发明人: HUANG LAN

    摘要: The present invention provides convergent processes for preparing (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, and (-)-beta-elemene fluoride and analogues thereof. Also provided are intermediates useful for preparing (-)-beta-elemene. The present invention further provides novel compositions based on analogues of (-)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, (-)-beta-elemene fluoride and methods for the treatment of cancer, such as brain tumor, lung cancer, breast cancer, prostate cancer, ovarian cancer, colorectal cancer, gastric intestional cancer, and stomach cancer. The inventors propose a combination therapy using 1) one or more of the following anti-cancer agents: including, but not limited to, Cisplatin, 5-FU, Taxol, Taxol derivatives, and any anti-cancer agent, and 2) one or more of the following (-)-beta-elemene and its analogs, including (-)-beta-elemene, (-)-beta-elemenol, (-)-beta-elemenol, (-)-beta-elemene fluoride, and their analogs, and (-)-beta-elemene's intermediate in its chemical synthesis, for the treatment of cancer, especially for the treatment of brain tumor, lung cancer, ovarian cancer, bladder cancer, cervical cancer,. colon cancer, breast cancer, and prostate cancer.

    摘要翻译: 本发明提供( - ) - β-榄香烯,( - ) - β-元素,( - ) - β-榄香烯和( - ) - β-榄香烯氟化物及其类似物的收敛方法。 还提供了可用于制备( - ) - β-榄香烯的中间体。 本发明还提供了基于( - ) - β-榄香烯,( - ) - β-元素,( - ) - β-榄香烯,( - ) - β-榄香烯氟化物类似物和治疗癌症的新方法 ,例如脑肿瘤,肺癌,乳腺癌,前列腺癌,卵巢癌,结肠直肠癌,胃肠癌和胃癌。 本发明人提出了使用以下1种或多种抗癌药物的组合疗法:包括但不限于顺铂,5-FU,紫杉醇,紫杉醇衍生物和任何抗癌剂,以及2)一种或多种 ( - ) - β-榄香烯,( - ) - β-榄香烯,( - ) - β-榄香烯,( - ) - β-榄香烯氟化物和 他们的类似物和( - ) - β-榄香烯在其化学合成中的中间体,用于治疗癌症,特别是用于治疗脑肿瘤,肺癌,卵巢癌,膀胱癌,子宫颈癌。 结肠癌,乳腺癌和前列腺癌。

    ORGANOCATALYSTS AND METHODS OF USE IN CHEMICAL SYNTHESIS
    2.
    发明申请
    ORGANOCATALYSTS AND METHODS OF USE IN CHEMICAL SYNTHESIS 审中-公开
    化学合成中的有机物和使用方法

    公开(公告)号:WO2006007586A1

    公开(公告)日:2006-01-19

    申请号:PCT/US2005/023691

    申请日:2005-06-30

    IPC分类号: C07D211/08

    摘要: The present invention pertains generally to compositions comprising organocatalysts that facilitate stereo-selective reactions and the method of their synthesis and use. Particularly, the invention relates to metal-free organocatalysts for facilitation of stereo-­selective reactions, and the method of their synthesis and use. These compounds have the structure of the Formulas (I) and (II). Where X is independently selected from CH 2 , N-R a , O, S or C=O; Y is CH 2 , N-R a , O, S or C=O, with the proviso that at least one of X or Y is CH 2 , and preferably both of X and Y are CH 2 ; R a is H, an optionally substituted C 1 -C 12 alkyl, preferably an optionally substituted C 1 -C 6 alkyl including a C 3 -C 6 cyclic alkyl group, or an optionally substituted aryl group, preferably an optionally substituted phenyl group; R b is H, an optionally substituted C 1 -C 12 alkyl, preferably an optionally substituted C 1 -C 6 acyclic or a a C 3 -C 6 cyclic alkyl group, CHO, N(Me)O, CO(S)R a or the group of Formula (III). Where R c and R d are each independently H, F, C1, an optionally substituted C 1- C 20 alkyl, preferably an optionally substituted C 1 -C 12 alkyl, more preferably a C 1 -C 6 alkyl, and an optionally substituted aryl group, or together R c and R d form an optionally substituted carbocyclic or optionally substituted heterocyclic ring; R 1 is OH, OR, NR'R", NHC(=O)R, NHSO 2 R; R 2 is H, F, C1, an optionally substituted C 1- C 20 alkyl, preferably an optionally substituted C 1 ­C 6 alkyl, an optionally substituted aryl group or a =O group (which establishes a carbonyl group with the carbon to which =O is attached; R 3 is H, OH, F, C1, Br, I, Cl, an optionally substituted C 1 -C 20 alkyl, alkenyl or alkynyl ("hydrocarbyl") group, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl, such that the carbon to which R 3 is attached has an R or S configuration; R is H, an optionally substituted C 1 -C 20 alkyl, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl group, R' and R" are each independently H, an optionally substituted C 1 -C 20 alkyl group, preferably an optionally substituted C 1 -C 6 alkyl, or an optionally substituted aryl group; or together R' and R" form an optionally substituted heterocyclic, preferably a 4 to 7 membered optionally substituted heterocyclic group or an optionally substituted heteroaryl ring with the nitrogen to which R' and R" are attached; and wherein said compound is free from a metal catalyst.

    摘要翻译: 本发明通常涉及促进立体选择性反应的有机催化剂及其合成和使用方法的组合物。 特别地,本发明涉及促进立体选择性反应的无金属有机催化剂及其合成和使用方法。 这些化合物具有式(I)和(II)的结构。 其中X独立地选自CH 2,N-R a,O,S或C = O; Y是CH 2,NR a,O,S或C = O,条件是X或Y中的至少一个是CH 2 2 >,并且优选X和Y两者都是CH 2 2; R a是H,任选取代的C 1 -C 12烷基,优选任选取代的C 1 -C 12 - 包括C 3 -C 6环烷基的C 6 -C 6烷基或任选取代的芳基,优选任选取代的苯基; R b是H,任选取代的C 1 -C 12烷基,优选任选取代的C 1 -C 12烷基, C 6不饱和环或C 3 -C 6环烷基,CHO,N(Me)O,CO(S)R SUP > III或式(III)的基团。 其中R 0和R d各自独立地为H,F,C 1,任选取代的C 1 -C 20 >烷基,优选任选取代的C 1 -C 12烷基,更优选C 1 -C 12烷基,更优选C 1 -C 12 - 烷基和任选取代的芳基,或一起R和C和R d形成任选取代的碳环或任选取代的杂环; R 1是OH,OR,NR'R“,NHC(= O)R,NHSO 2 R; R 2是H,F ,C 1,任选取代的C 1 -C 20烷基,优选任选取代的C 1 -C 6烷基 ,任选取代的芳基或= O基团(其中与O连接的碳上形成羰基; R 3是H,OH,F,Cl,Br,I,Cl ,任选取代的C 1 -C 20烷基,烯基或炔基(“烃基”)基团,优选任选取代的C 1 -C C 6 -C 6烷基或任选取代的芳基,使得R 3连接的碳具有R或S构型; R是H,任选取代的C

    CARBONYL COMPOUNDS AND THEIR USE AS FRAGRANCES
    4.
    发明申请
    CARBONYL COMPOUNDS AND THEIR USE AS FRAGRANCES 审中-公开
    羰基及其作为增香剂使用

    公开(公告)号:WO00027784A1

    公开(公告)日:2000-05-18

    申请号:PCT/EP1999/008282

    申请日:1999-10-30

    摘要: The invention relates to carbonyl compounds of the general structure (I) where the rest R is hydrogen or an alkyl group with between 1 and 5 carbon atoms, the rests R and R independently of each other are hydrogen or an alkyl group with between 1 and 3 carbon atoms and one of the positions C-1/C-2, C-2/C-3 or C-1/C-6 has a C=C double bond, and the rest R is either hydrogen or, if the C=C double bond is situated in position C-2/C-3, hydrogen or an alkyl group with between 1 and 3 carbon atoms. The above compounds are characterized by interesting fragrance notes of great intensity and are suitable for use as fragrances in, for example, cosmetic preparations, technical products or perfumed spirits.

    摘要翻译: 通式结构(I)其中基团R <1>是氢或具有1至5个碳原子,基团的烷基的羰基化合物中,R <2>和R <3>独立地是氢或具有1至3个C的烷基 平均原子,并且在所述位置中的一个C-1 / C-2,C-2 / C-3或C-1 / C-6是一个C = C双键存在且R <4>是氢或 - 条件是在位置C-2 / C-3中的C = C双键坐在 - 氢或具有1至3个碳原子的烷基,其特征在于,有趣香料以极大的光彩和适合用作香料,如 在化妆品制剂,工业产品或含酒精的香水。