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    Method for producing chiral or enantiomer-enriched beta-amino acids, aldehydes, ketones and gama-amino alcohols
    7.
    发明申请
    Method for producing chiral or enantiomer-enriched beta-amino acids, aldehydes, ketones and gama-amino alcohols 审中-公开
    制备手性或对映体富集的β-氨基酸，醛，酮和氨基醇的方法

    公开(公告)号：US20070123589A1

    公开(公告)日：2007-05-31

    申请号：US10582671

    申请日：2004-11-25

    申请人： Walther Jary ,  Ben De Lange ,  Quirinus Broxterman ,  Peter Pochlauer ,  Marcellas Van Der Sluis ,  Patrick Uiterweerd ,  Heinz Falk ,  Gerhard Zuckerstatter

    发明人： Walther Jary ,  Ben De Lange ,  Quirinus Broxterman ,  Peter Pochlauer ,  Marcellas Van Der Sluis ,  Patrick Uiterweerd ,  Heinz Falk ,  Gerhard Zuckerstatter

    IPC分类号： A61K31/195 ,  A61K31/13 ,  C07C227/02

    CPC分类号： C07C213/00 ,  C07C231/12 ,  Y02P20/55 ,  C07C215/28 ,  C07C233/18 ,  C07C233/31 ,  C07C233/47

    摘要： The invention relates to an improved method for producing chiral or enantiomer-enriched beta amino acids, -aldehydes, -ketones and gamma-amino alcohols, during which an allyl amine of formula (I), in which: R1 represents an alkyl radical, a cycloalkyl radical, an alkyl radical, a heterocycle radical or a condensed or bridged ring system; R2, R3, R4 and R5, independent of one another, can represent H or an alkyl radical, a cyclo alkyl radical, an aryl radical, a heterocycle radical or a condensed or bridged ring system or radicals R1, R2, R3 and R4, together, form ring systems that can optionally contain one or more heteroatoms, whereby radicals R1, R2, R3, R4 and R5 can be substituted once or a number of times, and; R6 represents H or an N-protective group, is transformed; a) by ozonolysis in a solvent and; b) subsequent decomposition of the peroxide-containing solution by means of an oxidizing agent or reductive reprocessing, into the corresponding amino compound of formula (II), in which R1, R2, R3, R4 and R6 are defined as above, and; A, according to the reprocessing, represents a radical of formula COOH, —C(OH)R5 or —C(O)R5, whereby R5 is defined as above.

    摘要翻译： 本发明涉及制备手性或对映体富集的β氨基酸，醛，酮和γ-氨基醇的改进方法，其中式（I）的烯丙胺，其中：R1表示烷基， 环烷基，烷基，杂环基或稠合或桥连环系; R 2，R 3，R 4和R 5彼此独立地可以表示H或烷基，环烷基，芳基，杂环基或稠合或桥接的环系或基团R 1，R 2，R 3和R 4， 一起形成可任选地含有一个或多个杂原子的环系，其中基团R 1，R 2，R 3，R 4和R 5可以被取代一次或多次， R6表示H或N-保护基，被转化; a）通过溶剂中的臭氧分解; b）随后通过氧化剂或还原再加工将含过氧化物的溶液分解成相应的式（II）的氨基化合物，其中R 1，R 2，R 3，R 4和R 6如上定义; 根据后处理，A代表式COOH，-C（OH）R 5或-C（O）R 5的基团，其中R 5如上所定义。

    Increased enantioselectivity of lipase catalyzed transesterification of alkynols with vinyl esters
    9.
    发明授权
    Increased enantioselectivity of lipase catalyzed transesterification of alkynols with vinyl esters 失效
    脂肪酶催化的炔基酯与乙烯基酯的酯交换增加了对映选择性

    公开(公告)号：US5639662A

    公开(公告)日：1997-06-17

    申请号：US529712

    申请日：1995-09-18

    申请人： Herbert Mayrhofer ,  Irma Wirth ,  Peter Pochlauer

    发明人： Herbert Mayrhofer ,  Irma Wirth ,  Peter Pochlauer

    IPC分类号： C12P41/00

    CPC分类号： C12P41/004

    摘要： Process for enhancement of enantioselectivity in the enzymatic separation of (R)- and (S)-enantiomers of an asymmetric alkynol, a lipase and in the presence of at least one vinyl ester, in which the acid component has at least 4 C atoms, an organic solvent and with the addition of water. Also disclosed is a process for enhancement of enantioselectivity in the enzymatic separation of (R)- and (S)-enantiomers of an alcohol with the aid of the abovementioned vinyl ester under addition of a second vinyl ester having at least 2 C atoms less in the alkyl chain than the vinyl ester used as esterifying agent.

    摘要翻译： 用于增强不对称炔醇，脂肪酶和至少一种乙烯基酯的（R） - 和（S） - 对映异构体的酶分离中的对映体选择性的方法，其中酸组分具有至少4个C原子， 有机溶剂和加入水。 还公开了一种通过在上述乙烯基酯的帮助下，在加入具有至少2个C原子的第二乙烯基酯的情况下，在醇的（R） - 和（S） - 对映体的酶分离中增强对映体选择性的方法 烷基链比乙烯基酯用作酯化剂。