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14 条记录 (耗时 0.043 秒)

    Method for producing 4-cyano-2-aminomethylthiazole
    8.
    发明授权
    Method for producing 4-cyano-2-aminomethylthiazole 有权
    4-氰基-2-氨基甲基噻唑的制备方法

    公开(公告)号：US06639081B1

    公开(公告)日：2003-10-28

    申请号：US10031703

    申请日：2002-04-30

    申请人： Monika Knopp ,  Stefan Koser ,  Bernd Schaefer

    发明人： Monika Knopp ,  Stefan Koser ,  Bernd Schaefer

    IPC分类号： C07D27704

    CPC分类号： C07D277/56

    摘要： The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ib in which n=1 or 2 and for n=1, X is chloride, bromide, triflate and hydrogen sulfate and for n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula II is stirred with a cysteine ester of the formula III, in which R1 is branched or linear C1-10-alkyl or where n=0, 1 or 2 and R2 is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.

    摘要翻译： 本发明涉及制备2-氨基甲基-4-氰基噻唑及其盐，其中n = 1或2，n = 1，X为氯化物，溴化物，三氟甲磺酸酯和硫酸氢盐，n = 2，X为 硫酸盐，其包括其中式II的氨基腈与式III的半胱氨酸酯一起搅拌的方法步骤，其中R 1是支链或直链的C 1-10 - 烷基或其中n = 0,1或2， 2>是在0℃至80℃的碱存在下，在惰性溶剂中的支链或直链C 1 -C 10 C 10 - 烷基或C 1 -C 4 - 烷氧基或C 1 -C 4 - 二烷基氨基，直到反应基本上进行 以及式Ia和Ib的化合物。

    Method for producing esters of triazolopyrimidine derivatives free of enantiomers using vinylesters with lipase
    9.
    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

    申请人： Friedhelm Balkenhohl ,  Stefan Koser ,  Nicholas John Holman

    发明人： Friedhelm Balkenhohl ,  Stefan Koser ,  Nicholas John Holman

    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
    10.
    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

    申请人： Nicholas John Holman ,  Stefan Koser

    发明人： Nicholas John Holman ,  Stefan Koser

    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。