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    POLYENE POLYKETIDES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS A PHARMACEUTICAL
    2.
    发明申请
    POLYENE POLYKETIDES, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS A PHARMACEUTICAL 审中-公开
    聚烯烃聚合物，其生产工艺及其作为药物的使用

    公开(公告)号：WO2004065401A1

    公开(公告)日：2004-08-05

    申请号：PCT/CA2004/000068

    申请日：2004-01-21

    申请人： ECOPIA BIOSCIENCES INC. ,  BACHMANN, Brian, O. ,  MCALPINE, James, B. ,  ZAZOPOULOS, Emmanuel ,  FARNET, Chris, M.

    发明人： BACHMANN, Brian, O. ,  MCALPINE, James, B. ,  ZAZOPOULOS, Emmanuel ,  FARNET, Chris, M.

    IPC分类号： C07H15/203

    CPC分类号： C07H15/203 ,  C07C215/24 ,  C07C225/14 ,  C07C235/28 ,  C07C237/16 ,  C07C279/22 ,  C07C305/14 ,  C07C2601/10 ,  C07C2601/14 ,  C07H15/10 ,  C07H15/18 ,  C07H15/26 ,  C12P7/42 ,  C12P11/00 ,  C12P13/001 ,  C12P13/02 ,  C12P19/44 ,  C12R1/465 ,  Y10S435/886

    摘要： This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis ; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.

    摘要翻译： 本发明涉及新类型的多烯聚酮化合物，其药学上可接受的盐和衍生物，以及获得化合物的方法。 获得这些化合物的一种方法是通过培养新的链霉菌链霉菌菌株; 另一种方法涉及在转化的宿主细胞中表达生物合成途径基因。 本发明还涉及用于制备这些化合物的新型链霉菌链霉菌菌株，以及这些化合物及其药学上可接受的盐和衍生物作为药物的用途，特别是其作为真菌细胞生长抑制剂和癌细胞生长的用途。 本发明还涉及包含这些新型聚酮化合物或其药学上可接受的盐或衍生物的药物组合物。 最后，本发明涉及参与这些新型聚酮化合物的生物合成的新型多核苷酸序列及其编码的蛋白质。

    STEREOSELECTIVE SYNTHESIS OF CIS-4-METHYLSPHINGOSINE AND DERIVATIVES THEREOF
    5.
    发明申请
    STEREOSELECTIVE SYNTHESIS OF CIS-4-METHYLSPHINGOSINE AND DERIVATIVES THEREOF 审中-公开
    CIS-4-甲基鞘氨醇及其衍生物的选择性合成

    公开(公告)号：WO2012150292A1

    公开(公告)日：2012-11-08

    申请号：PCT/EP2012/058102

    申请日：2012-05-03

    申请人： HUMBOLDT-UNIVERSITÄT zu BERLIN ,  ARENZ, Christoph ,  PROKSCH, Denny

    发明人： ARENZ, Christoph ,  PROKSCH, Denny

    IPC分类号： C07C215/24 ,  C07F9/38 ,  C07D263/06 ,  C07D309/12

    CPC分类号： C07C215/24 ,  C07D263/06 ,  C07D309/12 ,  C07F9/091 ,  C07F9/3808 ,  Y02P20/55

    摘要： The invention provides for synthesis of a (S-R) dihydroxy-amino-methylalkylene characterized by the general formula I, or its R-S diastereomer, wherein R1 is CH 2 OH or CH 2 -CH 2 OH, and R2 is C 2 to C 20 alkyl, whereby a compound characterized by the general formula II, with R3, R4 and R5 being protecting groups for amino and hydroxyl functions, respectively, is used as a starting material. The invention further provides novel intermediates for syntheses of, and analogues to, cis -4-methylsphingosine.

    摘要翻译： 本发明提供合成特征为通式I或其RS非对映异构体的（SR）二羟基 - 氨基 - 甲基亚烷基，其中R 1为CH 2 OH或CH 2 -CH 2 OH，且R 2为C 2至C 20烷基， 通式II，其中R3，R4和R5分别作为氨基和羟基官能团的保护基用作起始原料。 本发明还提供了用于顺式-4-甲基鞘氨醇的合成和类似物的新型中间体。

    AN IMPROVED PROCESS FOR THE PREPARATION OF TERBINAFINE INTERMEDIATE
    7.
    发明申请
    AN IMPROVED PROCESS FOR THE PREPARATION OF TERBINAFINE INTERMEDIATE 审中-公开
    一种改进的中草药中间体制剂的改进方法

    公开(公告)号：WO2005058794A1

    公开(公告)日：2005-06-30

    申请号：PCT/IN2003/000394

    申请日：2003-12-17

    申请人： NATCO PHARMA LIMITED ,  PULLA REDDY, Muddasani ,  VENKIAH CHOWDARY, Nannapaneni ,  RAJASEKHARA REDDY, Peddi

    发明人： PULLA REDDY, Muddasani ,  VENKIAH CHOWDARY, Nannapaneni ,  RAJASEKHARA REDDY, Peddi

    IPC分类号： C07C213/08

    CPC分类号： C07C213/00 ,  C07C213/10 ,  C07C215/24

    摘要： This application discloses an improved process for the preparation of N-methyl-N-(1-naphthylmethyl)-6,6-dimethyl-2-hydroxyheptan-4-ynyl-1-amine, a key intermediate used in the synthesis of terbinafine ((E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethanamine). Process is involving converting tertiary-butylacetylene to its Grignard derivative via transmetallation using lower alkylmagnesium halides and treating it with 1-[N-methyl-N-(1-naphtylmethyl)amino]-2,3-epoxypropane at -10°C to -20°C, slowly heating the reaction mass to reflux temperature and quenching of reaction mass with ammonium chloride to give the compound of the formula-I as crystalline solid.

    摘要翻译： 本申请公开了一种改进的制备N-甲基-N-（1-萘基甲基）-6,6-二甲基-2-羟基庚-4-炔-1-胺的方法，该方法是用于合成特比萘芬的关键中间体 （E）-N-（6,6-二甲基-2-庚烯-4-炔基）-N-甲基-1-萘甲胺）。 方法是通过使用低级烷基卤化镁通过金属转移将叔丁基乙炔转化成格利雅衍生物，并在-10℃下用1- [N-甲基-N-（1-萘甲基）氨基] -2,3-环氧丙烷处理， 20℃，缓慢加热反应物质至回流温度，用氯化铵淬灭反应物质，得到式I化合物，为结晶固体。

    PROCESS FOR THE SYNTHESIS OF CHIRALLY PURE beta -AMINO-ALCOHOLS
    9.
    发明申请
    PROCESS FOR THE SYNTHESIS OF CHIRALLY PURE beta -AMINO-ALCOHOLS 审中-公开
    合成纯度β-氨基醇的方法

    公开(公告)号：WO03050063A2

    公开(公告)日：2003-06-19

    申请号：PCT/US0238119

    申请日：2002-11-26

    申请人： WYETH CORP

    发明人： KREFT ANTHONY FRANK ,  ANTANE MADELENE MIYOKO ,  COLE DEREK CECIL ,  KUBRAK DENNIS MARTIN ,  RESNICK LYNN ,  STOCK JOSEPH RAYMOND ,  WANG ZHENG

    IPC分类号： A61K31/381 ,  C07B53/00 ,  C07B61/00 ,  C07C209/00 ,  C07C213/00 ,  C07C215/08 ,  C07C227/04 ,  C07C229/08 ,  C07C247/12 ,  C07D227/12 ,  C07D263/26 ,  C07D333/32 ,  C07D333/34 ,  C07C

    CPC分类号： C07C215/20 ,  C07B2200/07 ,  C07C215/08 ,  C07C215/24 ,  C07C215/28 ,  C07C215/56 ,  C07C229/08 ,  C07C229/28 ,  C07C229/30 ,  C07C229/36 ,  C07C247/12 ,  C07C323/63 ,  C07D263/26 ,  C07D333/34

    摘要： A process is provided for preparing chirally pure S-enantiomers of alpha -amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the Formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an alpha -azido acid; h) reducing the alpha -azido acid to the alpha -amino acid; and i) recrystallizing the alpha -amino acid to the chirally pure alpha -amino acid. A process is also provided for preparing chirally pure S-enantiomers of beta -amino alcohols further comprising the steps of reducing the crude alpha -amino acid to the beta -amino alcohol and recrystallizing the beta -amino alcohol to the chirally pure beta -amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl beta -amino alcohols further comprising the steps of sulfonylating the beta -amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl beta -amino alcohols.

    摘要翻译： 提供了制备α-氨基酸的手性纯的S-对映异构体的方法，包括以下步骤：a）由式（R）2CH（CH 2）n CH 2 X的烷基卤制备有机金属试剂; b）将有机金属试剂加入到二氧化碳中，得到羧酸; c）在叔胺碱存在下用酰氯，三氯化磷，酸酐或亚硫酰氯活化羧酸; d）使步骤c）的产物与S-4-苄基-2-恶唑烷酮的碱金属盐反应; e）用强非亲核碱处理步骤d）的产物以形成烯醇化物阴离子; f）用2,4,6-三异丙基苯磺酰叠氮化物捕获烯醇化阴离子，得到恶唑烷酮叠氮化物; g）用碱水溶液水解恶唑烷酮叠氮化物，得​​到α-叠氮酸; h）将α-叠氮酸还原成α-氨基酸; 和i）将α-氨基酸重结晶到手性纯的α-氨基酸。 还提供了制备β-氨基醇的手性纯的S-对映异构体的方法，该方法还包括将α-氨基酸粗制还原成β-氨基醇并将β-氨基醇重结晶至手性纯的β-氨基醇 。 还提供了制备N-磺酰基β-氨基醇的手性纯S对映异构体的方法，其还包括用5-氯 - 噻吩-2-磺酰卤磺酰化β-氨基醇的步骤; 并重结晶得到手性纯的N-磺酰基β-氨基醇。