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12 条记录 (耗时 0.017 秒)

    Method for producing esters of triazolopyrimidine derivatives free of enantiomers using vinylesters with lipase
    1.
    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。

    Resolution of racemates of primary and secondary heteroatom-substitued amines by enzyme-catalyzed acylation
    5.
    发明授权
    Resolution of racemates of primary and secondary heteroatom-substitued amines by enzyme-catalyzed acylation 失效
    通过酶催化酰化拆分初级和次级杂原子取代的胺的外消旋体

    公开(公告)号：US06214608B1

    公开(公告)日：2001-04-10

    申请号：US08875417

    申请日：1997-07-28

    申请人： Friedhelm Balkenhohl ,  Klaus Ditrich ,  Christoph Nübling

    发明人： Friedhelm Balkenhohl ,  Klaus Ditrich ,  Christoph Nübling

    IPC分类号： C12P4100

    CPC分类号： C12P41/007 ,  C12P13/02

    摘要： A process for preparing optically active primary and secondary heteroatom-substituted amines from the corresponding racemates, which comprises a) enantioselective acylation of a racemic heteroatom-substituted amine with an ester whose acid component carries a fluorine, nitrogen, phosphorus, oxygen or sulfur atom in the vicinity of the carbonyl carbon, in the presence of a hydrolase, b) separation of the mixture of optically active heteroatom-substituted amine and optically active acylated heteroatom-substituted amine to obtain one enantiomer of the heteroatom-substituted amine, c) if required isolation of the other enantiomer of the heteroatom-substituted amine from the acylated heteroatom-substituted amine by amide cleavage.

    摘要翻译： 从相应的外消旋物制备光学活性的伯和仲杂原子取代的胺的方法，其包括：a）外消旋杂原子取代的胺与其酸成分在其中含有氟，氮，磷，氧或硫原子的酯的对映选择性酰化 在水解酶的存在下，羰基碳的邻近，b）分离光学活性的杂原子取代的胺和光学活性的酰化的杂原子取代的胺的混合物以获得杂原子取代的胺的一个对映异构体，c）如果需要的话， 的通过酰胺切割从酰化的杂原子取代的胺的杂原子取代的胺的另一个对映异构体。

    Resolution of the racemates of primary and secondary amines by enzyme-catalyzed acylation
    6.
    发明授权
    Resolution of the racemates of primary and secondary amines by enzyme-catalyzed acylation 失效
    通过酶催化酰化拆分伯胺和仲胺的外消旋体

    公开(公告)号：US5728876A

    公开(公告)日：1998-03-17

    申请号：US596238

    申请日：1996-03-11

    申请人： Friedhelm Balkenhohl ,  Bernhard Hauer ,  Wolfgang Ladner ,  Uwe Pressler ,  Christoph Nubling

    发明人： Friedhelm Balkenhohl ,  Bernhard Hauer ,  Wolfgang Ladner ,  Uwe Pressler ,  Christoph Nubling

    IPC分类号： C12P13/02 ,  C12P41/00 ,  C12R1/38 ,  C07C231/02 ,  C07C231/16

    CPC分类号： C12P13/02 ,  C12P41/007

    摘要： A process for producing optically active primary and secondary amines from the corresponding racemates is characterised in that (a) a racemic amine is enantioselectively acylated in the presence of a hydrolase with an ester whose acid component bears a fluorine, nitrogen, oxygen or sulphur atom at the proximity of the carbonyl carbon atom; (b) the mixture of optically active amine and optically active acylated amine is separated so that an enantiomer of amine is produced; (c) if desired the other enantiomer of the amine is extracted from the acylated amine by amide cleavage.

    摘要翻译： PCT No.PCT / EP94 / 03102 Sec。 371日期：1996年3月11日 102（e）1996年3月11日PCT PCT 1994年9月16日PCT公布。 出版物WO95 / 08636 日期：1995年3月30日从相应的外消旋体制备光学活性伯胺和仲胺的方法的特征在于：（a）外消旋胺在水解酶存在下被对映选择性酰化，其中酸组分含有氟，氮， 在羰基碳原子附近的氧或硫原子; （b）分离光学活性胺和光学活性酰化胺的混合物，使得产生胺的对映异构体; （c）如果需要，胺的另一对映异构体通过酰胺裂解从酰化胺中提取。

    Preparation of calcium L-ascorbate 2-phosphate
    8.
    发明授权
    Preparation of calcium L-ascorbate 2-phosphate 失效
    L-抗坏血酸钙2-磷酸钙的制备

    公开(公告)号：US5420302A

    公开(公告)日：1995-05-30

    申请号：US102745

    申请日：1993-08-06

    申请人： Klaus Kaiser ,  Friedhelm Balkenhohl ,  Joachim Paust

    发明人： Klaus Kaiser ,  Friedhelm Balkenhohl ,  Joachim Paust

    IPC分类号： C07F9/655 ,  C07F9/06

    CPC分类号： C07F9/65515

    摘要： A process for isolating the calcium salt of ascorbyl 2-monophosphate from aqueous alkaline reaction mixtures as are obtained on reaction of ascorbic acid with a molar excess of phosphorus oxychloride in the presence of a tertiary amine while maintaining a pH of from 12 to 13 during the reaction by means of an aqueous alkali metal hydroxide solution, which comprisesa) starting from a reaction mixture which has been obtained by reacting ascorbic acid with phosphorus oxychloride in the presence of pyridine while maintaining a pH of from 12 to 13 by means of an aqueous potassium hydroxide solution,b) precipitating, as potassium magnesium phosphate, the phosphate ions which have been formed in this reaction by means of magnesium chloride in amounts of about 1 mol per mol of phosphate ions,c) removing the potassium magnesium phosphate,d) distilling the remaining aqueous solution to remove the pyridine together with part of the water,e) reacting the resulting aqueous solution with calcium chloride andf) isolating the calcium salt of ascorbyl 2-monophosphate which crystallizes thereby, or first distilling the pyridine-water mixture according to step (d) from the reaction mixture obtained in step (a) and thereafter carrying out steps (b), (c), (e) and (f).

    摘要翻译： 在碱性反应混合物水溶液中分离抗坏血酸2-单磷酸钙的方法，该方法是在叔胺存在下使抗坏血酸与摩尔过量的三氯氧化磷反应得到的，同时保持pH为12至13 通过碱金属氢氧化物水溶液进行反应，其包括a）从吡啶存在下使抗坏血酸与三氯氧磷反应获得的反应混合物开始，同时通过水溶液保持pH为12至13 氢氧化钾溶液，b）以磷酸镁钾的形式沉淀在该反应中通过氯化镁形成的磷酸根离子，其量为每摩尔磷酸根离子约1摩尔，c）除去磷酸镁钾，d） 蒸馏剩余的水溶液以与一部分水一起除去吡啶，e）使所得水溶液与calciu反应 m），和f）分离由此结晶的2-抗坏血酸的钙盐，或者首先从步骤（a）获得的反应混合物中蒸馏出根据步骤（d）的吡啶 - 水混合物，然后进行步骤（b） ，（c），（e）和（f）。