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    PROCESS FOR THE PRODUCTION OF ASYMMETRIC EPOXIDES UNDER NON-AQUEOUS CONDITIONS AND CATALYTIC COMPOSITION FOR USE THEREIN
    1.
    发明申请
    PROCESS FOR THE PRODUCTION OF ASYMMETRIC EPOXIDES UNDER NON-AQUEOUS CONDITIONS AND CATALYTIC COMPOSITION FOR USE THEREIN 审中-公开
    在非水溶液条件下生产不对称环氧化物的方法及其使用的催化组合物

    公开(公告)号：WO2004085415A1

    公开(公告)日：2004-10-07

    申请号：PCT/GB2004/001277

    申请日：2004-03-25

    申请人： STYLACATS LIMITED ,  ROBERTS, Stanley, Michael ,  PITTS, Michael, Robert

    发明人： ROBERTS, Stanley, Michael ,  PITTS, Michael, Robert

    IPC分类号： C07D301/12

    CPC分类号： C07D301/12

    摘要： A process for the asymmetric epoxidation of α,β-unsaturated carbonyl or sulphonyl compounds comprising : providing, in the absence of an aqueous phase, a catalyst/reagent composition comprising a poly-amino acid catalyst effective for catalysing the asymmetric epoxidation reaction, the poly-amino acid catalyst encapsulating an expoxidation reagent effective for epoxidation of α,β-unsaturated carbonyl or sulphonyl compounds; contacting the catalyst/reagent composition with an α,β-unsaturated carbonyl or sulphonyl compound substrate under conditions effective to provide at least partial asymmetric epoxidation of the substrate by the epoxidation reagent; and recovering the resulting asymmetric epoxide.

    摘要翻译： α，β-不饱和羰基或磺酰化合物的不对称环氧化方法，包括：在不存在水相的情况下，提供包含有效催化不对称环氧化反应的聚氨基酸催化剂的催化剂/试剂组合物，聚 包封有效用于α，β-不饱和羰基或磺酰基化合物环氧化的过氧化试剂的氨基酸催化剂; 在有效地通过环氧化试剂提供底物至少部分不对称环氧化的条件下使催化剂/试剂组合物与α，β-不饱和羰基或磺酰基化合物底物接触; 并回收所得的不对称环氧化物。

    ASYMMETRIC EPOXIDES, THEIR SYNTHESIS AND USE
    4.
    发明申请
    ASYMMETRIC EPOXIDES, THEIR SYNTHESIS AND USE 审中-公开
    不对称环氧化合物，它们的合成和用途

    公开(公告)号：WO1996033183A1

    公开(公告)日：1996-10-24

    申请号：PCT/GB1996000953

    申请日：1996-04-19

    申请人： CHIROSCIENCE LIMITED ,  ROBERTS, Stanley, Michael ,  ADGER, Brian, Michael

    发明人： CHIROSCIENCE LIMITED

    IPC分类号： C07D303/32

    CPC分类号： C07D303/48 ,  C07C227/08 ,  C07C231/02 ,  C07D303/32

    摘要： A process for preparing an optically-enriched chiral epoxide of formula (I), wherein R , R and R are each independently selected from H, R, R-CO- and R-O-CO-, each R independently being substantially a hydrocarbon group of up to 20 carbon atoms, and X is an alkyl or cycloalkyl group of up to 10 carbon atoms, provided that -CO-X is not enolisable, which comprises the asymmetric epoxidation of a corresponding prochiral alkene of the formula (II): R R C=CR -CO-X, by reaction with an oxidant in the presence of a chiral catalyst. Many optically-enriched epoxides (I) are novel.

    摘要翻译： 制备式（I）的光学富集手性环氧化物的方法，其中R 1，R 2和R 3各自独立地选自H，R，R-CO-和RO-CO-， 每个R独立地基本上是至多20个碳原子的烃基，X是至多10个碳原子的烷基或环烷基，条件是-CO-X不是可烯化的，其包括对应的前手性烯烃的不对称环氧化 式（II）的化合物：R 1 R 2 C = CR 3 -CO-X，通过在手性催化剂的存在下与氧化剂反应。 许多光学富集的环氧化物（I）是新颖的。

    BICYCLIC CYLOPENTANONE AND CYCLOPENTENONE DERIVATIVES AS POTENT ACTIVATORS OF HSF
    5.
    发明申请
    BICYCLIC CYLOPENTANONE AND CYCLOPENTENONE DERIVATIVES AS POTENT ACTIVATORS OF HSF 审中-公开
    作为HSF的激活剂的双环CYLOPENTANONE和环戊烯酮衍生物

    公开(公告)号：WO2004013117A1

    公开(公告)日：2004-02-12

    申请号：PCT/GB2003/003410

    申请日：2003-08-06

    申请人： CHARTERHOUSE THERAPEUTICS LTD. ,  ROBERTS, Stanley, Michael ,  SANTORO, Gabriella, Maria ,  EVANS, Paul

    发明人： ROBERTS, Stanley, Michael ,  SANTORO, Gabriella, Maria ,  EVANS, Paul

    IPC分类号： C07D307/93

    CPC分类号： C07D307/93 ,  C07D209/52

    摘要： A compound of formula (I), (II), (III) or (IV); wherein R 1 and R 2 are each, independently, hydrogen or an alkyl group containing 1-4 carbon atoms; R 3 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1-3 carbon atoms; R 4 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; R 5 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; Y is hydrogen or a halogen; X is oxygen or NR 6 ; R 6 is hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms, -COOR 7 , -SO 2 R 7 , -OSO 2 R 7 , or -COR 7 ; and R 7 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-20 carbon atoms.

    摘要翻译： 式（I），（II），（III）或（IV）的化合物; 其中R 1和R 2各自独立地为氢或含有1-4个碳原子的烷基; R 3是氢或含有1-3个碳原子的取代或未取代的烷基或链烯基; R 4是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子; R 5是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子; Y是氢或卤素; X是氧或NR 6; R 6是氢，取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子，-COOR 7 ，-SO 2 R 7，-OSO 2 R 7或-COR 7; 并且R 7是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-20个碳原子。

    CHIRAL COMPOUNDS AND THEIR USE
    7.
    发明申请
    CHIRAL COMPOUNDS AND THEIR USE 审中-公开
    CHIRAL COMPOUNDS及其使用

    公开(公告)号：WO1994007888A1

    公开(公告)日：1994-04-14

    申请号：PCT/GB1993002008

    申请日：1993-09-27

    申请人： CHIROSCIENCE LIMITED ,  ROBERTS, Stanley, Michael ,  OLIVO, Horacio, F. ,  McCAGUE, Raymond

    发明人： CHIROSCIENCE LIMITED

    IPC分类号： C07D309/30

    CPC分类号： C07C49/753 ,  C07C49/707

    摘要： 4-Hydroxy- delta -lactones are useful intermediates in the preparation of inhibitors of the enzyme (HMG-CoA reductase) that is rate-limiting in cholesterol biosynthesis. They are prepared from synthons of the formula (A) wherein either Y is H and - &cir& _- &cir& _- &cir& _ is a double bond or epoxide, or Y is optionally-blocked OH (above the ring, opposite to Z) and - &cir& _- &cir& _- &cir& _ is a single bond; and Z is an organic group.

    摘要翻译： 4-羟基-δ-内酯是制备胆固醇生物合成中速率限制酶（HMG-CoA还原酶）的抑制剂的有用中间体。 它们由式（A）的合成物制备，其中Y为H且 - 为C 1 -C 6烷基，或者Y为双键或环氧化物，或Y为任选封闭的OH（环上方为Z） - ＆cir＆_-＆cir＆_-＆cir＆_是单一债券; Z是有机基团。

    IMPROVEMENTS IN PHARMACEUTICALLY USEFUL COMPOUNDS
    8.
    发明申请
    IMPROVEMENTS IN PHARMACEUTICALLY USEFUL COMPOUNDS 审中-公开
    药物有效化合物的改进

    公开(公告)号：WO2004013077A2

    公开(公告)日：2004-02-12

    申请号：PCT/GB2003/003413

    申请日：2003-08-06

    申请人： CHARTERHOUSE THERAPEUTICS LTD ,  ROBERTS, Stanley, Michael ,  SANTORO, Gabriella, Maria ,  HAPPE, Alan, Michael ,  DAUVERNE, Jerome ,  JADHAV, Vasudev

    发明人： ROBERTS, Stanley, Michael ,  SANTORO, Gabriella, Maria ,  HAPPE, Alan, Michael ,  DAUVERNE, Jerome ,  JADHAV, Vasudev

    IPC分类号： C07C49/00

    CPC分类号： C07C323/59 ,  C07C45/673 ,  C07C49/647 ,  C07C49/653 ,  C07C49/657 ,  C07C49/753 ,  C07C205/45 ,  C07C225/20 ,  C07C233/32 ,  C07C233/76 ,  C07C271/24 ,  C07C271/36 ,  C07C271/56 ,  C07C271/66 ,  C07C311/20 ,  C07C311/53 ,  C07C323/43 ,  C07C2601/08 ,  C07C2601/10

    摘要： A compound of formula (I) or (II): wherein A is hydrogen or CR 1 R 2 ; Y and Z are each, independently, hydrogen or a halogen;X is -NR 4 R 5 , or R 7 ; R 1 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1-4 carbon atoms; when X is -NR 4 R 5 , R 2 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; when X is R 7 , R 2 is an unsubstituted alkyl, alkenyl or alkynyl group, or a substituted or unsubstituted aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; R 3 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; R 4 is hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms, -COOR 8 , or -COR 8 ; R 5 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1-5 carbon atoms; R 7 is an unsubstituted alkyl, alkenyl, or alkynyl group, that contains 1-4 carbon atoms; and, R 8 is an unsubstituted or halo-substituted alkyl, aryl, or aralkyl group, that contains 1-12 carbon atoms.

    摘要翻译： 式（I）或（II）的化合物：其中A是氢或CR 1 R 2; Y和Z各自独立地为氢或卤素; X为-NR 4 R 5或R 7; R 1是氢或含有1-4个碳原子的取代或未取代的烷基或链烯基; 当X是-NR 4 R 5时，R 2是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包括至少一个杂原子，并且含有 1-12个碳原子; 当X是R 7时，R 2是未取代的烷基，烯基或炔基，或取代或未取代的芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子，并含有1 -12个碳原子; R 3是任选地在其碳骨架中包含至少一个杂原子并且含有1-12个碳原子的取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基， R 4是氢，取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子，-COOR 8 或-COR 8; R 5是氢或含有1-5个碳原子的取代或未取代的烷基或链烯基; R 7是含有1-4个碳原子的未取代的烷基，烯基或炔基; 并且R 8是含有1-12个碳原子的未取代或卤素取代的烷基，芳基或芳烷基。