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    Process for preparing heterocyclic (R)- and (S)-cyanohydrins
    8.
    发明授权
    Process for preparing heterocyclic (R)- and (S)-cyanohydrins 失效
    制备杂环（R） - 和（S） - 氰基醇的方法

    公开(公告)号：US07052885B2

    公开(公告)日：2006-05-30

    申请号：US10325922

    申请日：2002-12-23

    申请人： Peter Poechlauer ,  Wolfgang Skranc ,  Herbert Mayrhofer ,  Irma Wirth ,  Rudolf Neuhofer ,  Herfried Griengl ,  Martin Fechter

    发明人： Peter Poechlauer ,  Wolfgang Skranc ,  Herbert Mayrhofer ,  Irma Wirth ,  Rudolf Neuhofer ,  Herfried Griengl ,  Martin Fechter

    IPC分类号： C12P17/00 ,  C12P17/02 ,  C12P17/04 ,  C12P17/06 ,  C12P17/18

    CPC分类号： C12P13/004 ,  C12P17/00 ,  C12P17/04

    摘要： A process for preparing enantiomer-enriched heterocyclic (R)- and (S)-cyanohydrins of the formula (I), where R1, R2, R3, R4 independently of one another are H, an unsubstituted or substituted C1–C24-alkyl, alkenyl or alkynyl radical, where one or more carbon atoms in the chain can be replaced by an oxygen atom, a nitrogen atom, a sulfur atom, an SO or an SO2 group, an unsubstituted or substituted aryl or heteroaryl radical or heterocyclic radical or halogen, hydroxyl, NR5R6, acetyl, oxo, C1–C6-carbalkoxy, C1–C6-carbalkoxyamino, COOR7, cyano, amide, benzoylamino or NO2,R5 and R6 are H, C1–C6-alkyl radical, phenyl radical, benzyl radical or COOR7, or together form a C2–C8-alkylene or heteroalkylene radical,R7 is H or C1–C6-alkyl,n is 0, 1, 2 or 3,X, Y and Z can be an unsubstituted or substituted carbon atom or a radical selected from the group consisting of N, O, S or NR5R6, where R5 and R6 are as defined above, SO or SO2, and at least one of the radicals X, Y and Z is not a carbon atom, where the compounds of the formula (I) can have one or more double bonds in the ring, with the proviso that in a 5-membered ring the double bond is not conjugated with the —C(OH)CN-group, and/or can be anellated and/or bridged,by reacting a ketone of the formula (II), where R1, R2, R3, R4, X, Y, Z and n have the meanings above, with an (R)- or (S)-hydroxynitrile lyase in an organic, aqueous or two-phase system, or in emulsion, in the presence of a cyanide group donor.

    摘要翻译： 制备式（I）的对映异构体富集的杂环（R） - 和（S） - 氰基醇的方法，其中R 1，R 2，R 3，R 4彼此独立地是H，未取代或取代的C 1 - 链烯基或炔基，其中链中的一个或多个碳原子可以被氧原子，氮原子，硫原子，SO或 SO 2 2基团，未取代或取代的芳基或杂芳基或杂环基或卤素，羟基，NR 5 R 6，乙酰基，氧代C 1 -C 6 - 亚烷基氧基，C 1 -C 6 - 烷氧基氨基，COOR 7，氰基，酰胺，苯甲酰氨基或NO 2，R 5和R 6是H C 1 -C 6 - 烷基，苯基，苄基或COOR 7，或一起形成C 1 -C 6 - 8亚烷基或杂亚烷基，R 7是H或C 1 -C 6 - 烷基，n是0,1,2或3，X，Y 并且Z可以是未取代或取代的碳原子或选自它的基团 由N，O，S或NR5R6组成的基团，其中R 5和R 6如上定义，SO或SO 2，并且基团X，Y和Z中的至少一个不是碳 原子，其中式（I）的化合物可以在环中具有一个或多个双键，条件是在5元环中双键不与-C（OH）CN-基团共轭，并且 /或可以通过使式（II）的酮（其中R 1，R 2，R 3，R 4，X，Y，Z和n具有上述含义）与（R） - 或（ S） - 羟基腈裂解酶在有机，水相或两相体系中，或在乳液中，在氰化物基团给体存在下。

    R-hydroxynitrillyases havign improved substrate tolerance and the use thereof
    9.
    发明申请
    R-hydroxynitrillyases havign improved substrate tolerance and the use thereof 失效
    R-hydroxynitrillyases有利于改善底物耐受性及其用途

    公开(公告)号：US20060105434A1

    公开(公告)日：2006-05-18

    申请号：US10548271

    申请日：2004-02-24

    申请人： Wolfgang Skranc ,  Anton Glieder ,  Karl Gruber ,  Roland Weis ,  Ruud Luiten

    发明人： Wolfgang Skranc ,  Anton Glieder ,  Karl Gruber ,  Roland Weis ,  Ruud Luiten

    IPC分类号： C12P13/04 ,  C12P13/00 ,  C12N9/88

    CPC分类号： C12P13/004 ,  C12N9/88

    摘要： The invention related to R-hydroxynitrillyases from the family of Rosaceae that are characterized by an improved substrate tolerance and increased stability. In the active center of the R-hydroxynitrillyases either a) an alanine group is substituted by glycine, valine, leucine, isoleucine, or phenylalanine or b) a phenylalanine group is substituted by alanine, glycine valine, leucine or isoleucine, or c) a leucine group is substituted by alanine, glycine, valine, isoleucine or phenylalanine, or d) an isoleucine group is substituted by alanine, glycine, valine, leucine or phenylalanine. The invention also relates to the use of these lyases in the production of enantiomer-pure R- or S-cyanohydrines.

    摘要翻译： 本发明涉及来自蔷薇科家族的R-羟基亚硝酸酯酶，其特征在于改善的底物耐受性和增加的稳定性。 或者a）丙氨酸被甘氨酸，缬氨酸，亮氨酸，异亮氨酸或苯丙氨酸取代，或b）苯丙氨酸被丙氨酸，甘氨酸缬氨酸，亮氨酸或异亮氨酸取代，或c） 亮氨酸被丙氨酸，甘氨酸，缬氨酸，异亮氨酸或苯丙氨酸取代，或d）异亮氨酸被丙氨酸，甘氨酸，缬氨酸，亮氨酸或苯丙氨酸取代。 本发明还涉及这些裂解酶在制备对映异构体纯的R-或S-氰基中的用途。

    Process for preparing protected, enantiomer-enriched cyanohydrins by in-situ derivatization
    10.
    发明授权
    Process for preparing protected, enantiomer-enriched cyanohydrins by in-situ derivatization 失效
    通过原位衍生制备保护的富含对映异构体的氰醇的方法

    公开(公告)号：US06909011B2

    公开(公告)日：2005-06-21

    申请号：US10325923

    申请日：2002-12-23

    申请人： Wolfgang Skranc ,  Peter Poechlauer ,  Irma Wirth ,  Rudolf Neuhofer ,  Herbert Mayrhofer

    发明人： Wolfgang Skranc ,  Peter Poechlauer ,  Irma Wirth ,  Rudolf Neuhofer ,  Herbert Mayrhofer

    IPC分类号： C12P13/00 ,  C12R1/91 ,  C07C253/16 ,  C12P13/16

    CPC分类号： C12P13/004

    摘要： A process for preparing protected, enantiomer-enriched cyanohydrins of the formula where R1 and R2 independently of one another can be an unsubstituted, monosubstituted or polysubstituted C1-C20-alkyl, C5-C20-aryl, C5-C20-heteroaryl, C5-C20-alkaryl, C5-C20-alkylheteroaryl or C5-C20-aralkyl radical or an unsubstituted, monosubstituted or polysubstituted C5-C20-heterocycle, or C5-C20-alkylheterocycle or together can be an unsubstituted or substituted C4-C20-alkylene radical, which can contain one or more heteroatoms in the chain, or one of the radicals is hydrogen, and R3 can be an unsubstituted or substituted C1-C20-alkyl, C5-C20-aryl or C5-C20-heteroaryl radical, by reacting an aldehyde or ketone of the formula where R1 and R2 are defined as above, in the presence of an (R)- or (S)-hydroxynitrile lyase in an organic, aqueous or 2-phase system or in emulsion at a temperature of −5 to +40° C. with a carbonic ester nitrile of the formula where R3 is defined as above.

    摘要翻译： 制备具有下式的受保护的对映异构体富含氰醇的方法其中R 1和R 2彼此独立地可以是未取代的，单取代的或多取代的C 1 -C 20 - 烷基 C 5 -C 20 - 芳基，C 5 -C 20 - 杂芳基，C 5 - C 20 -C 20 - 烷芳基，C 5 -C 20 - 烷基杂芳基或C 5 -C 或是未取代的单取代或多取代的C 5 -C 20 - 杂环或C 5 - -C 20 - 烷基杂环或一起可以是未取代或取代的C 4 -C 20 - 亚烷基，其可以含有一个或多个杂原子 在链中，或者一个基团是氢，并且R 3可以是未取代或取代的C 1 -C 20 - 烷基，C 5 C 20 -C 20 - 芳基或C 5 -C 20 - 杂芳基，通过使下式的醛或酮反应其中R1和R2 在有机，水相或两相体系中的（R） - 或（S） - 羟基腈裂解酶存在下，或在-5至+ 40℃的温度下与碳酸酯 腈，其中R3如上定义。