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    • 1. 发明申请
    • PROCESS FOR PREPARING 3-SUBSTITUTED 2-ALKENALS, IN PARTICULAR PRENAL
    • 制备3-取代的2-ALKENALS,特别是预处理的方法
    • WO2013076226A1
    • 2013-05-30
    • PCT/EP2012/073422
    • 2012-11-23
    • BASF SE
    • SCHAUB, ThomasBRUNNER, BernhardEBEL, KlausPACIELLO, Rocco
    • C07C45/00C07C35/04C07C47/20C07C47/21C07C45/29
    • C07C45/66C07C45/002C07C45/29C07C47/21C07C47/20
    • The present invention to a process for preparing 2-alkenals of the formula (I) in which R 1 is selected from hydrogen and C 1 -C 4 -alkyl; and R 2 is selected from hydrogen, C 1 -C 12 -alkyl, C 2 -C 12 -alkenyl, C 4 -C 8 -cycloalkyl and C 6 -C- 10 aryl, wherein C 1 -C 12 -alkyl and C 1 -C 12 -alkenyl may be substituted with C 5 -C 7 -cycloalkyl or C 5 -C 7 -cylcoalkenyl; comprising dehydrogenating an alkenol of the formula (II), an alkenol of the formula (III) or a mixture thereof, wherein R 1 and R 2 are each as defined above, wherein the alkenol II, the alkenol III or a mixture thereof is brought into contact with a catalytic system comprising at least one ligand and a metal compound selected from ruthenium(II) compounds and iridium(I) compounds, and wherein the hydrogen formed during the dehydrogenation is removed from the reaction mixture by: i) reaction with a reoxidant selected from C 3 -C 12 -alkanones, C 4 -C 9 -cycoalkanones, benzaldehyde and mixtures thereof; and/or ii) purely physical means.
    • 本发明涉及一种制备式(I)的2-烯烃的方法,其中R 1选自氢和C 1 -C 4 - 烷基; 并且R 2选自氢,C 1 -C 12 - 烷基,C 2 -C 12 - 链烯基,C 4 -C 8 - 环烷基和C 6 -C 10芳基,其中C 1 -C 12 - 烷基和C 1 -C 12 - 烯基可以被C 5- C7-环烷基或C5-C7-环烯基; 包括使式(II)的烯醇,式(III)的烯醇或其混合物脱氢,其中R 1和R 2各自如上所定义,其中链烯醇II,链烯醇III或其混合物接触 具有包含至少一种配体和选自钌(II)化合物和铱(I))化合物的金属化合物的催化体系,并且其中通过以下步骤从反应混合物中除去脱氢过程中形成的氢:i)与选择的再氧化剂反应 C 3 -C 12烷基酮,C 4 -C 9 - 环烷基酮,苯甲醛及其混合物; 和/或ii)纯粹的物理手段。
    • 4. 发明申请
    • SYNTHESIS OF (-)-BETA-ELEMENE, (-)-BETA-ELEMENAL, (-)-BETA-ELEMENOL, (-)-BETA-ELEMENE FLUORIDE AND THEIR ANALOGUES, INTERMEDIATES AND COMPOSITION AND USES THEREOF
    • ( - ) - 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
    • WO2006016912A3
    • 2007-02-15
    • PCT/US2005014699
    • 2005-05-02
    • LONG RANGE INTERNAT USA LTD INHUANG LAN
    • HUANG LAN
    • C07C13/19A61K31/015A61K31/025A61K31/045A61K31/11C07C21/18C07C35/17C07C47/20C07C47/21
    • C07C49/647C07B2200/07C07C1/324C07C13/19C07C33/14C07C35/18C07C45/30C07C47/21C07C49/557C07C2601/14C07C2601/16
    • 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.
    • 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。
    • 5. 发明申请
    • IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS
    • 有机化合物的改善或有关
    • WO2016091894A1
    • 2016-06-16
    • PCT/EP2015/079008
    • 2015-12-08
    • GIVAUDAN SA
    • BAUMGARTNER, CorinneFLACHSMANN, Felix
    • C07C33/02C07C33/18C07C47/20C11B9/00
    • C07C43/23C07C69/738C11B9/0003C11B9/0015
    • A fragrance precursor represented by the formula (1) wherein the wavy bond is indicating an unspecified configuration of the adjacent double bond, X and Y together represent a double bond to a carbon atom which is bearing R 1 and R 2 , with R 1 = H, methyl, acetyl or C 1 -C 3 alkoxycarbonyl (e.g. ethoxycarbonyl); and R 2 = phenyl optionally substituted with up to 3 (i.e. 0, 1, 2 or 3) groups selected from C 1 -C 4 alkyl (e.g. methyl, ethyl, iso-propyl, tert-butyl), vinyl, hydroxy, C 1 -C 3 alkoxy (e.g. ethoxy), and -O-CH 2 -O-, e.g. R 2 is benzo[d][1,3]dioxol-5-yl, 4-methylphenyl, 4-methoxyphenyl, 4-vinylphenyl or 3-ethoxy-4-hydroxyphenyl or R 2 = naphthyl, (naphthyl)methyl, 1,1,2,4,4,8-hexamethyl-1,2,3,4-tetrahydronaphthalen-7-yl, or 1,1,2,4,4,-pentamethyl-1,2,3,4-tetrahydronaphthalen-7-yl or R 2 = COR3, wherein R 3 is H, C 1 -C 10 alkoxy (e.g. ethoxy, 1-(3,3-dimethylcyclohexyl)ethoxy), C 1- C 4 alkyl (e.g. methyl, ethyl, propyl, iso-propyl, tert-butyl), e.g. R 2 is formyl, acetyl, ethoxycarbonyl, 1-(3,3-dimethylcyclohexyl)ethoxycarbonyl; or wherein X is OR 4 , with R 4 being H, alkyl or alkenyl, and Y is OR 5 , with R 5 being alkyl or alkenyl; the compound being useful as a perfume ingredient.
    • 由式(1)表示的香料前体,其中波状键表示相邻双键的未指定构型,X和Y一起表示与带有R 1和R 2的碳原子的双键,其中R 1 = H,甲基 ,乙酰基或C 1 -C 3烷氧基羰基(如乙氧羰基); 并且R2 =任选被至多3个(即0,1,2或3)选自C 1 -C 4烷基(例如甲基,乙基,异丙基,叔丁基),乙烯基,羟基,C 1 -C 3烷氧基 (例如乙氧基)和-O-CH2-O-,例如 R2是苯并[d] [1,3]二氧杂环戊烯-5-基,4-甲基苯基,4-甲氧基苯基,4-乙烯基苯基或3-乙氧基-4-羟基苯基或R 2 =萘基,(萘基)甲基, 2,4,4,8-六甲基-1,2,3,4-四氢萘-7-基或1,1,2,4,4 - 五甲基-1,2,3,4-四氢萘-7-酮, 或R 2 = COR 3,其中R 3为H,C 1 -C 10烷氧基(例如乙氧基,1-(3,3-二甲基环己基)乙氧基),C 1 -C 4烷基(例如甲基,乙基,丙基,异丙基,叔丁基 ),例如 R2是甲酰基,乙酰基,乙氧基羰基,1-(3,3-二甲基环己基)乙氧基羰基; 或其中X为OR4,其中R4为H,烷基或烯基,Y为OR5,R5为烷基或烯基; 该化合物可用作香料成分。