Method for producing esters of triazolopyrimidine derivatives free of enantiomers using vinylesters with lipase
    2.
    发明授权
    Method for producing esters of triazolopyrimidine derivatives free of enantiomers using vinylesters with lipase 失效
    使用具有脂肪酶的乙烯基酯制备不含对映异构体的三唑并嘧啶衍生物的酯的方法

    公开(公告)号:US06234811B1

    公开(公告)日:2001-05-22

    申请号:US09319875

    申请日:1999-06-14

    IPC分类号: C12P1718

    CPC分类号: C12P41/004 C12P17/182

    摘要: A process for preparing enantiomerically pure esters of the formula I (Ia and Ib) where the substituents have the following meanings: R1 hydrogen or substituted or unsubstituted C1-C6-alkyl, C1-C6-alkoxy or Cl-C6-alkanoyl, R2 and R3 independently of one another hydrogen or substituted or unsubstituted C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkanoyl, C1-C6-alkylthio, C1-C6-alkylsulfinyl or C1-C6-alkylsulfonyl, R4 and R5 R4≠R5 and independently of one another hydrogen or substituted or unsubstituted C1-C6-alkyl or R4 and R5 form together with the carbon atoms to which they are bonded a substituted or unsubstituted C3-C6-cycloalkylidene, R6 substituted or unsubstituted aryl, C1-C20-alkyl, C3-C20-alkenyl, C3-C20-alkynyl, C1-C20-alkoxy-C1-C20-alkyl comprises converting racemic compounds of the formula II, where the substituents R1 to R5 have the abovementioned meanings, with a lipase or esterase in the presence of vinyl esters of the formula III, where R6 has the abovementioned meaning, and R7 is hydrogen or methyl, into compounds of the formula I.

    摘要翻译: 制备式I(Ia和Ib)的对映异构体纯的酯的方法,其中取代基具有以下含义:R 1氢或取代或未取代的C 1 -C 6 - 烷基,C 1 -C 6 - 烷氧基或C 1 -C 6 - 烷酰基,R 2和R 3独立地 的另一个氢或取代或未取代的C 1 -C 6 - 烷基,C 1 -C 6 - 烷氧基,C 1 -C 6 - 烷酰基,C 1 -C 6 - 烷硫基,C 1 -C 6烷基亚磺酰基或C 1 -C 6烷基磺酰基,R 4和R 5 R 4 并且彼此独立地是氢或取代或未取代的C 1 -C 6 - 烷基或R 4和R 5与它们所连接的碳原子一起形成取代或未取代的C 3 -C 6 - 亚环烷基,R 6取代或未取代的芳基,C 1 -C 20 - 烷基 C 3 -C 20烯基,C 3 -C 20炔基,C 1 -C 20烷氧基-C 1 -C 20烷基,其中取代基R 1至R 5具有上述含义的式II外消旋化合物与脂肪酶或酯酶 存在式III的乙烯基酯,其中R 6具有上述含义,并且R 7是氢 或甲基转化成式I的化合物。

    Process for the preparation of 7-alkoxyalkyl-1,2,4-triazolo[1,5-A] pyrimidine derivatives
    3.
    发明授权
    Process for the preparation of 7-alkoxyalkyl-1,2,4-triazolo[1,5-A] pyrimidine derivatives 失效
    制备7-烷氧基烷基-1,2,4-三唑并[1,5-A]嘧啶衍生物的方法

    公开(公告)号:US06225469B1

    公开(公告)日:2001-05-01

    申请号:US09242465

    申请日:1999-02-17

    IPC分类号: C07D48704

    CPC分类号: C07D487/04

    摘要: An improved process for the preparation of 1,2,4-triazolo[1,5-a]pyrimidine compounds comprising the reaction involving a compound of formula II and a compound of formula III in the presence of an oxidizing agent and a reducing agent, wherein a metal salt is added to form a complex with the oxidized reducing agent produced in the process, and this complex is separated from the desired product.

    摘要翻译: 一种用于制备1,2,4-三唑并[1,5-a]嘧啶化合物的改进方法,其包括在氧化剂和还原剂存在下包括式II化合物和式III化合物的反应,其中a 加入金属盐以与该方法中产生的氧化还原剂形成络合物,并将该络合物与所需产物分离。

    Method for producing alcohols free of enantiomers
    4.
    发明授权
    Method for producing alcohols free of enantiomers 失效
    生产不含对映异构体的醇的方法

    公开(公告)号:US06255087B1

    公开(公告)日:2001-07-03

    申请号:US09331404

    申请日:1999-06-21

    IPC分类号: C12P1716

    CPC分类号: C12P17/182

    摘要: A process for preparing enantiomerically pure alcohols of the formula I (Ia or Ib) where the substituents have the following meanings: R1 hydrogen or substituted or unsubstituted C1-C6-alkyl, C1-C6-alkoxy or C1-C6-alkanoyl, R2 and R3 independently of one another hydrogen or substituted or unsubstituted C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkanoyl, C1-C6-alkylthio, C1-C6-alkylsulfinyl or C1-C6-alkylsulfonyl, R4 substituted or unsubstituted C1-C6-alkyl, C3-C8-cycloalkyl, which comprises reducing compounds of the formula II where the substituents R1 to R4 have the abovementioned meanings  in aqueous solution in the presence of a carbon source and of a microorganism or of a reducing agent, of a cofactor and of an enzyme, to compounds of the formula I.

    摘要翻译: 制备式I(Ia或Ib)的对映异构体纯的醇的方法,其中取代基具有以下含义:R 1氢或取代或未取代的C 1 -C 6 - 烷基,C 1 -C 6 - 烷氧基或C 1 -C 6 - 烷酰基,R 2和R 3独立地 的一个或多个取代或未取代的C 1 -C 6 - 烷基,C 1 -C 6 - 烷氧基,C 1 -C 6 - 烷酰基,C 1 -C 6 - 烷硫基,C 1 -C 6烷基亚磺酰基或C 1 -C 6烷基磺酰基, - 烷基,C 3 -C 8 - 环烷基,其包括在辅助因子的碳源和微生物或还原剂存在下的水溶液中取代基R 1至R 4具有上述含义的式II的还原性化合物 和酶,与式I化合物反应。