Process for the preparation of D-asparagine derivatives
    12.
    发明授权
    Process for the preparation of D-asparagine derivatives 有权
    D-天冬酰胺衍生物的制备方法

    公开(公告)号:US06420166B2

    公开(公告)日:2002-07-16

    申请号:US09834129

    申请日:2001-04-12

    IPC分类号: C12P1320

    摘要: The present invention provides a process for the preparation of D-asparagine derivatives of formula I wherein R1 is an amino protecting group and R2 is an alkyl, a substituted alkyl or a group of formula A R3(OCH2CH2)n—  A wherein R3 is hydrogen or an lower alkyl group and n is 1, 2 or 3, which process comprises reacting a compound of formula II wherein R1 and R2 are as defined above, with a protease in an aqueous solution at a pH of 6.0-7.5 and an organic solvent, and subsequently extracting the enantiomeric pure product of formula I. Compounds of formula I can be used as intermediates in the production of antibacterial substances.

    摘要翻译: 本发明提供了制备式I的D-天冬酰胺衍生物的方法,其中R1是氨基保护基,R2是烷基,取代的烷基或式A的基团,其中R3是氢或低级烷基,n是1 ,2或3,该方法包括使R1和R2如上所定义的式II化合物与蛋白酶在pH为6.0-7.5的水溶液和有机溶剂中反应,随后萃取式对映体纯的产物 I.式I化合物可用作生产抗菌物质的中间体。

    NOVEL PHOSPHINE LIGANDS
    19.
    发明申请
    NOVEL PHOSPHINE LIGANDS 审中-公开
    新的磷酸盐配体

    公开(公告)号:US20090326253A1

    公开(公告)日:2009-12-31

    申请号:US12557553

    申请日:2009-09-11

    IPC分类号: C07F15/04

    摘要: The invention is concerned with new phosphine ligands of the formula I whereinR1 and R2 are independently of each other alkyl, aryl, cycloalkyl or heteroaryl, said alkyl, aryl, cycloalkyl or heteroaryl may be substituted by alkyl, alkoxy, halogen, hydroxy, amino, mono- or dialkylamino, aryl, —SO2—R7, —SO3−, —CO—NR8R8′, carboxy, alkoxycarbonyl, trialkylsilyl, diarylalkylsilyl, dialkylarylsilyl or triarylsilyl;R3 is alkyl, cycloalkyl, aryl or heteroaryl; R4′ and R4 signify independently of each other hydrogen, alkyl or optionally substituted aryl; or R4′ and R4 together with the C-atom they are attached to form a 3-8-membered carbocyclic ring; dotted line is absent or is present and forms a double bond; R5 and R6 are independently of each other hydrogen, alkyl or aryl; or linked together to form a 3-8-membered carbocyclic ring or an aromatic ring; R7 is alkyl, aryl or NR8R8′; and R8 and R8′ are independently of each other hydrogen, alkyl or aryl;metal complexes with such ligands as well as the use of such metal complexes as catalysts in asymmetric reactions.

    摘要翻译: 本发明涉及式I的新膦配体,其中R 1和R 2彼此独立地为烷基,芳基,环烷基或杂芳基,所述烷基,芳基,环烷基或杂芳基可以被烷基,烷氧基,卤素,羟基,氨基 ,一或二烷基氨基,芳基,-SO 2 -R 7,-SO 3 - ,-CO-NR 8 R 8',羧基,烷氧基羰基,三烷基甲硅烷基,二芳基烷基甲硅烷基,二烷基芳基甲硅烷基或三芳基甲硅烷基; R3是烷基,环烷基,芳基或杂芳基; R4'和R4独立地表示氢,烷基或任选取代的芳基; 或R 4'和R 4与它们所连接的C原子一起形成3-8-元碳环; 虚线不存在或存在并形成双键; R5和R6彼此独立地为氢,烷基或芳基; 或连接在一起形成3-8元碳环或芳环; R7是烷基,芳基或NR8R8'; R8和R8'彼此独立地为氢,烷基或芳基; 与这种配体的金属络合物以及在不对称反应中使用这样的金属络合物作为催化剂。