METHOD FOR PREPARING (R)-PRAZIQUANTEL

    公开(公告)号:US20140370556A1

    公开(公告)日:2014-12-18

    申请号:US14471841

    申请日:2014-08-28

    发明人: Mingxin Qian

    摘要: The invention relates to a new method for preparing (R)-praziquantel. In the invention, by taking advantage of the high stereo selectivity, site selectivity and region selectivity of an enzyme, an intermediate of a pure optical and chiral (R)-praziquantel are obtained by means of the dynamic kinetic resolution of an enantiomer from the synthesized racemate or derivatives thereof, and the (R)-praziquantel is obtained by using various conventional and mature organic chemical reactions with higher yield. The method of the invention has the potential advantages of easily available raw materials, low cost, environmentally safer process and convenience for large-scale production. Also, the purity of the end product can be more than 98%. By adopting the invention, the quality of the product is improved and a basis for developing high quality of active pharmaceutical ingredients and formulations is established, and thus the pending industrial problem of purifying praziquantel over 30 years becomes solvable.

    Enzymatically catalyzed method of preparing mono-acylated polyols
    3.
    发明授权
    Enzymatically catalyzed method of preparing mono-acylated polyols 失效
    单酰化多元醇的酶催化方法

    公开(公告)号:US08715970B2

    公开(公告)日:2014-05-06

    申请号:US13496342

    申请日:2010-09-16

    IPC分类号: C12P7/62 C12N1/21

    CPC分类号: C12P7/62 C12N9/20 C12P41/004

    摘要: The present invention relates to a biocatalytic method of preparing a mono-acylated polyol catalyzed by triacylglycerol lipase mutants, as for example derived from Candida antarctica lipase B (CALB); a biocatalytic method of enantioselectively preparing an asymmetric mono-acylated polyol, catalyzed by the same enzyme mutants; as well as the use of a mutated triacylglycerol lipase in a method of preparing mono-acylated polyols. The invention also provides novel mutants, coding sequences thereof, and recombinant microorganisms carrying said coding sequences.

    摘要翻译: 本发明涉及由三酰基甘油脂肪酶突变体催化的单酰化多元醇的生物催化方法,例如衍生自南极假丝酵母脂肪酶B(CALB); 通过相同的酶突变体催化的对映选择性制备不对称单酰化多元醇的生物催化方法; 以及在制备单酰化多元醇的方法中使用突变的三酰基甘油脂肪酶。 本发明还提供了新的突变体,其编码序列和携带所述编码序列的重组微生物。

    Method for the production of chiral secondary alcohols

    公开(公告)号:US20070196904A1

    公开(公告)日:2007-08-23

    申请号:US10592758

    申请日:2005-02-25

    IPC分类号: C12P13/00

    摘要: Disclosed is a method for producing chiral, secondary alcohols of formula (I), wherein A represents an aromatic, heterocyclic, or alicyclic ring or a ring system with 4 to 20 C atoms, n represents 0, 1, 2, 3, 4, or 5, R represents halogen, OH, an O— protective group, NO2, N,N—R2,R3 amine, R2 and R3 representing C1-C6 alkyl, phenyl, or benzyl, N,N—R2,R3-amino-C1-C6 alkyl, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C4 alkoxycarbonyl, or CN, and R1 represents N,N—R2,R3 amine, N,N—R2,R3-amino-C1-C6 alkyl, C1-C12 alkyl, C1-C6-haloalkyl, C1-C4 alkoxycarbonyl, C1-C6 alkoxy-C1-C6 alkyl, or a C2-C5 alkylene radical that forms a ring system along with the A radical. According to the inventive method, a) a ketone of formula (II) is optionally reduced to the corresponding racemic alcohol of formula (III) by means of an aliphatic C1-C6 alcohol in the presence of a transition metal catalyst and a base, and b) the alcohol of formula (III) is reacted to a mixture of (R) ester of formula (IV), wherein R4 represents H or C1-C5 alkyl, and (S) alcohol of formula (I) in the presence of an esterification catalyst and an acyl donor, whereupon the (S) alcohol is isolated from the reaction mixture by means of crystallization or distillation according to the aggregate state thereof.

    Catalytic antibodies
    9.
    发明授权
    Catalytic antibodies 失效
    催化抗体

    公开(公告)号:US07205136B1

    公开(公告)日:2007-04-17

    申请号:US08447924

    申请日:1995-05-23

    IPC分类号: C12N9/00

    摘要: A method for increasing the rate of chemical reactions involving the conversion of at least one reactant to at least one product involves contacting the reactant with an appropriate monoclonal antibody under conditions permitting the formation of a complex between the antibody and the reactant. The complexed reactant is converted to the product which is then released from the complex. The monoclonal antibody may employ a cofactor and may be directed to a known substrate of an enzyme. Methods for preparing such monoclonal antibodies are also disclosed.

    摘要翻译: 提高涉及将至少一种反应物转化为至少一种产物的化学反应速率的方法包括在允许抗体和反应物之间形成复合物的条件下使反应物与合适的单克隆抗体接触。 将络合的反应物转化成产物,然后将其从络合物中释放出来。 单克隆抗体可以使用辅因子并且可以被引导到酶的已知底物。 还公开了制备这种单克隆抗体的方法。