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    Beta-lactam antibiotics
    4.
    发明授权
    Beta-lactam antibiotics 失效
    β-内酰胺类抗生素

    公开(公告)号：US4200576A

    公开(公告)日：1980-04-29

    申请号：US862466

    申请日：1977-12-20

    申请人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    发明人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    IPC分类号： C07D499/66 ,  A61K31/415 ,  A61K31/42 ,  A61K31/43 ,  A61K31/435 ,  A61K31/505 ,  A61K31/535 ,  A61K31/545 ,  A61P31/04 ,  C07D233/38 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D501/20 ,  C07D501/57

    CPC分类号： C07D233/38 ,  C07D499/00 ,  Y02P20/55

    摘要： Antibacterially active and animal feedstuff supplement .beta.-lactam antibiotics of the formula ##STR1## in which R is H or --UR',U is O or S,R' is optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl or cycloalkyl,Z is ##STR2## R.sup.1 and R.sup.2 individually are hydrogen or, individually or together with the carbon atom to which they are bonded, are any of various radicals,A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## B is optionally substituted phenyl or is cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO.sub.2 or --CH.sub.2 --; andY is a group of the formula ##STR4## T is hydrogen, alkyl--CO--O--, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, hydroxyl or optionally substituted --S--phenyl, or is --S--Het, in whichHet is an optionally substituted heterocyclic 5-membered or 6-membered ring; and whereinE is hydrogen, a radical forming, with the carboxyl group to which it is attached, a carboxy ester group, a cation of a salt, or a protective group,or a hydrate thereof. A process is also given for converting R directly from H to UR' employing a base, a halogenating agent and R'UH .

    摘要翻译： 抗菌活性和动物饲料补充式为其中R为H或-UR'的式（I）的β-内酰胺抗生素，U为O或S，R'为任选取代的烷基，烯基，炔基，芳烷基，芳基或 环烷基，Z是R 1和R 2各自独立地是氢，或者与它们所键合的碳原子单独或一起是各种基团中的任何一个，A是-CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - 或 - B是任选取代的苯基或环己烯基或环己二烯基; X是S，O，SO，SO 2或-CH 2 - ; 并且Y是下式的基团：T是氢，烷基-CO-O-，吡啶鎓，氨基吡啶鎓，氨基甲酰氧基，叠氮基，氰基，羟基或任选取代的-S-苯基，或者是-S-Het，其中 Het是任选取代的杂环5元或6元环; 其中E为氢，与其连接的羧基形成的自由基为羧基酯基，盐的阳离子或保护基或其水合物。 还给出了使用碱，卤化剂和R'UH将R直接从H转化为UR'的方法。

    .beta.-Lactam antibiotics
    5.
    发明授权
    .beta.-Lactam antibiotics 失效
    β-内酰胺抗生素

    公开(公告)号：US4251524A

    公开(公告)日：1981-02-17

    申请号：US53655

    申请日：1979-06-29

    申请人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    发明人： Peter Feyen ,  Michael Preiss ,  Karl G. Metzger

    IPC分类号： C07D499/66 ,  A61K31/415 ,  A61K31/42 ,  A61K31/43 ,  A61K31/435 ,  A61K31/505 ,  A61K31/535 ,  A61K31/545 ,  A61P31/04 ,  C07D233/38 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D501/20 ,  C07D501/57 ,  A61K31/655

    CPC分类号： C07D233/38 ,  C07D499/00 ,  Y02P20/55

    摘要： Antibacterially active and animal feedstuff supplement .beta.-lactam antibiotics of the formula ##STR1## in which R is H or --UR',U is O or S,R' is optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl or cycloalkyl, ##STR2## R.sup.1 and R.sup.2 individually are hydrogen or, individually or together with the carbon atom to which they are bonded, are any of various radicals,A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## B is optionally substituted phenyl or is cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO.sub.2 or --CH.sub.2 --; andY is a group of the formula ##STR4## T is hydrogen, alkyl-CO-O-, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, hydroxyl or optionally substituted -S-phenyl, or is -S-Het,in whichHet is an optionally substituted heterocyclic 5-membered or 6-membered ring;and whereinE is hydrogen, a radical forming, with the carboxyl group to which it is attached, a carboxy ester group, a cation of a salt, or a protective group,or a hydrate thereof. A process is also given for converting R directly from H to UR' employing a base, a halogenating agent and R'UH.

    摘要翻译： 抗菌活性和动物饲料补充式为其中R为H或-UR'的式（I）的β-内酰胺抗生素，U为O或S，R'为任选取代的烷基，烯基，炔基，芳烷基，芳基或 环烷基，R 1和R 2分别是氢或者与它们所键合的碳原子单独或一起是各种基团中的任何一个，A是-CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - 或

    Process for the preparation of the (+)-antipode of (E)-1-cyclohexyl-4,4-dimethyl-3-hydroxy-2-(1,2,4-triazol-1-yl)-pent-1-en e
    6.
    发明授权
    Process for the preparation of the (+)-antipode of (E)-1-cyclohexyl-4,4-dimethyl-3-hydroxy-2-(1,2,4-triazol-1-yl)-pent-1-en e 失效
    （E）-1-环己基-4,4-二甲基-3-羟基-2-（1,2,4-三唑-1-基） - 戊-1-烯-1-酮的（+） - 对映体的制备方法， 恩

    公开(公告)号：US4789746A

    公开(公告)日：1988-12-06

    申请号：US835843

    申请日：1986-03-03

    申请人： Udo Kraatz ,  Peter Feyen

    发明人： Udo Kraatz ,  Peter Feyen

    IPC分类号： C07D249/08 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A process for the preparation of the (+)-antipode of (E)-1-cyclohexyl-4,4-dimethyl-3-hydroxy-2-(1,2,4-tri-azol-1-yl)-pent -1-ene of the formula ##STR1## which comprises reacting the (E)-isomer of 1-cyclohexyl-4,4-dimethyl-2-(1,2,4-triazol-1-yl)-pent-1-en-3-one of the formula ##STR2## with lithium aluminum hydride in the presence of an inert organic diluent and in the presence of a chiral amino alcohol at a temperature between -80.degree. C. and +50.degree. C. The (+)-antipode is produced in high selectivity, using (+)-N-methyl-ephedrine.

    摘要翻译： （E）-1-环己基-4,4-二甲基-3-羟基-2-（1,2,4-三唑-1-基） - 酮的（+） - 对映体的制备方法 -1-烯，其包括使1-环己基-4,4-二甲基-2-（1,2,4-三唑-1-基） - 戊-1-烯-1-酮的（E） - 异构体 在惰性有机稀释剂存在下，在手性氨基醇存在下，在-80℃至+ 50℃之间的温度下，将式（IMAGE）的3- ） - 使用（+） - N-甲基 - 麻黄碱以高选择性产生 -

    Preparation of phosphoric acid propargyl esters
    8.
    发明授权
    Preparation of phosphoric acid propargyl esters 失效
    磷酸炔丙酯的制备

    公开(公告)号：US4327040A

    公开(公告)日：1982-04-27

    申请号：US158032

    申请日：1980-06-09

    申请人： Gunter Arend ,  Peter Feyen

    发明人： Gunter Arend ,  Peter Feyen

    IPC分类号： A01N57/10 ,  B01J27/00 ,  C07B61/00 ,  C07F9/113 ,  C07F9/14 ,  C07F9/173

    CPC分类号： C07F9/173 ,  C07F9/113 ,  C07F9/1403

    摘要： A process for the preparation of a phosphoric acid propargyl ester of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is an aryl radical or a C.sub.1-4 -alkyl, C.sub.1-4 -alkenyl or C.sub.1-4 -alkynyl radical, andX, Y and Z each independently is oxygen or sulphur, comprising reacting a phosphoric acid monoester chloride or diester chloride with at least the equivalent amount of propargyl alcohol in a two-phase system in the presence of an inorganic base as an acid-trapping agent, and a catalyst comprising about 0.001 to 100 mol %, relative to the phosphoric acid ester chloride, of a tertiary amine or quaternary ammonium or phosphonium salt with at least 9 C atoms. Advantageously the catalyst is present in about 0.01 to 10 mol % relative to the phosphoric acid ester chloride and is a tertiary amine or quaternary ammonium salt, X, Y and Z are oxygen, R.sup.1 is propargyl and R.sup.2 is C.sub.1-4 -alkyl, the reaction is effected in the presence of methylene chloride, chloroform or toluene as solvent, the base is used in at least the equivalent amount and is selected from the group consisting of alkali metal hydroxides, alkaline earth metal hydroxides, alkali metal carbonates and alkaline earth metal carbonates.

    摘要翻译： 一种制备下式的磷酸炔丙酯的方法，其中R 1和R 2各自独立地是芳基或C 1-4 - 烷基，C 1-4 - 烯基或C 1-4 - 炔基，X ，Y和Z各自独立地是氧或硫，包括在无机碱作为酸捕获剂的存在下，使磷酸单酯氯化物或二酯氯化物与至少相当量的炔丙醇在两相体系中反应， 和相对于磷酸酯氯化物含有至少9个C原子的叔胺或季铵或鏻盐的约0.001至100摩尔％的催化剂。 有利地，催化剂相对于磷酸酯氯化物以约0.01至10mol％存在，并且是叔胺或季铵盐，X，Y和Z是氧，R 1是炔丙基，R 2是C 1-4 - 烷基， 反应在二氯甲烷，氯仿或甲苯作为溶剂的存在下进行，碱至少使用等量的碱金属氢氧化物，碱土金属氢氧化物，碱金属碳酸盐和碱土金属 碳酸盐

    Process for the preparation of oxiranes
    9.
    发明授权
    Process for the preparation of oxiranes 失效
    环氧乙烷的制备方法

    公开(公告)号：US4929735A

    公开(公告)日：1990-05-29

    申请号：US185211

    申请日：1988-04-22

    申请人： Wolf Reiser ,  Peter Feyen

    发明人： Wolf Reiser ,  Peter Feyen

    IPC分类号： C07D405/06 ,  C07D301/02 ,  C07D303/08 ,  C07D303/22 ,  C07D521/00

    CPC分类号： C07D303/22 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/08

    摘要： A process for the preparation of an oxirane of the formula ##STR1## in which X is 4-chlorobenzyl, 4-phenylphenoxy or 1H-(1,2,4)-triazolyl,comprising reacting dimethyl sulphate with an excess of dimethyl sulphide thereby to form trimethylsulphonium methyl-sulphate of the formula(CH.sub.3).sub.3 S.sym.CH.sub.3 SO.sub.4 .crclbar.,and without prior isolation reacting the trimethylsulphonium methyl-sulphate with a keytone of the formula ##STR2## in the presence of solid potassium hydroxide or sodium hydroxide in dimethyl sulphide at a temperature between 0.degree. C. and 50.degree. C.

    摘要翻译： 制备式“IMAGE”的环氧乙烷的方法，其中X是4-氯苄基，4-苯基苯氧基或1H-（1,2,4） - 三唑基，包括使硫酸二甲酯与过量的二甲基硫醚反应，从而 形成式（CH 3）3 S（+）CH 3 SO 4（ - ）的三甲基锍甲基硫酸盐，并且不经事先分离，在固体氢氧化钾或氢氧化钠存在下，使甲基硫酸三甲基锍与式 二硫化碳在0℃至50℃的温度下进行。

    Preparation of O,S-dimethyl-thiolophosphoric acid amide
    10.
    发明授权
    Preparation of O,S-dimethyl-thiolophosphoric acid amide 失效
    制备O，S-二甲基 - 硫代磷酸酰胺

    公开(公告)号：US4537730A

    公开(公告)日：1985-08-27

    申请号：US516167

    申请日：1983-07-21

    申请人： Peter Feyen ,  Hermann Seifert ,  Egon Kohler

    发明人： Peter Feyen ,  Hermann Seifert ,  Egon Kohler

    IPC分类号： C07F9/24

    CPC分类号： C07F9/24

    摘要： A simplified process for preparing the known insecticide 0,S-dimethylthiolphosphoric acid amide of the formula ##STR1## inexpensively, in high purity and with minimum waste water and gas which would have to be specially treated to avoid environmental pollution, comprises(a) contacting 0,0 dimethyl-thiophosphoric acid amide of the formula ##STR2## in which Me is sodium or potassium, separating the aqueous phase,(b) optionally adding an organic solvent to the aqueous phase, and reacting the mass with methyl bromide or methyl chloride thereby to form the 0,S-dimethyl-thiolphosphoric acid amide, and either(c) extracting the amide with a sparingly water-miscible solvent thereby to dissolve the amide, or(d) concentrating the reaction mixture from the methylation step (b), by distillation, until the alkali metal halide formed has separated out, and filtering off the alkali metal halide.

    摘要翻译： 制备低成本的已知杀虫剂0，S-二甲基硫代磷酸酰胺的简便方法是以高纯度和最少的废水和气体制备，该方法必须经过特殊处理以避免环境污染，其包括（a）接触 其中Me是钠或钾的0,0二甲基 - 硫代磷酸酰胺，其中Me是钠或钾，分离水相，（b）任选地向水相中加入有机溶剂，并使该物质与甲基溴或甲基氯 从而形成0S-二甲基 - 硫醇磷酸酰胺，和（c）用少量与水混溶的溶剂萃取酰胺，从而溶解酰胺，或（d）从甲基化步骤（b）浓缩反应混合物， 通过蒸馏，直到形成的碱金属卤化物分离出来，并过滤掉碱金属卤化物。