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    Process for preparing substituted urea derivatives
    1.
    发明授权
    Process for preparing substituted urea derivatives 失效
    制备取代脲衍生物的方法

    公开(公告)号：US4435567A

    公开(公告)日：1984-03-06

    申请号：US334470

    申请日：1981-12-28

    申请人： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Laszlo Simandi ,  Eva Somfai

    发明人： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Laszlo Simandi ,  Eva Somfai

    IPC分类号： C07D295/20 ,  C07C67/00 ,  C07C239/00 ,  C07C273/18 ,  C07C275/02 ,  C07C275/06 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07D213/75 ,  C07D217/06 ,  C07D235/32 ,  C07D275/06 ,  C07D277/82 ,  C07D285/12 ,  C07D285/135 ,  C07D295/215 ,  C07C127/00 ,  C07C127/15 ,  C07C127/17 ,  C07C127/19

    CPC分类号： C07D213/75 ,  C07C273/1809 ,  C07D217/06 ,  C07D235/32 ,  C07D277/82 ,  C07D285/135 ,  C07D295/215

    摘要： A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom may form a saturated or unsaturated heterocycle, or a condensed and/or substituted ring system, and said heterocycle or said condensed and/or substituted ring system may contain also a sulfo group,can be manufactured by reacting an amine of formula (II) ##STR2## with an N-carbamoyl-benzoic acid sulfimide derivative of formula (III) ##STR3## The disclosed N-acylating composition comprises of from 3 to 60% by weight, preferably of from 5 to 50% by weight sulfimide derivative of formula (III), of from 97 to 40% by weight, preferably of from 95 to 50% by weight solvent, and if desired, an organic or inorganic base.The disclosed N-acylating concentrate comprises of from 60 to 95.5% by weight N-acylating agent of formula (III) and of from 4.5 to 40% by weight additives.

    摘要翻译： 公开了用于制备取代的脲衍生物的方法，以及用于相同目的的组合物和浓缩物。 根据该方法，式（I）的取代脲衍生物其中R是氢，烷基，芳基，环烷基或芳烷基，R1和R2是氢，烷基，烯基，炔基，烷氧基，烷氧基，环烷基，芳烷基，烷氧基羰基 ，芳基或杂芳基，或R 1和R 2与相邻的氮原子一起可以形成饱和或不饱和的杂环或稠合和/或取代的环系，并且所述杂环或所述缩合和/或取代的环系可以含有磺基 可以通过使式（II）的胺与式（III）的N-氨基甲酰基 - 苯甲酸硫酰亚胺衍生物反应来制备。所公开的N-酰化组合物包含3至60重量％ ，优选为5至50重量％的式（III）的亚磺酰亚胺衍生物，为97至40重量％，优选为95至50重量％的溶剂，如果需要，为有机或无机碱。 所公开的N-酰化浓缩物包含60至95.5重量％的式（III）的N-酰化剂和4.5至40重量％的添加剂。

    Process for O-acylating phenol derivatives and acylating compositions for this purpose
    2.
    发明授权
    Process for O-acylating phenol derivatives and acylating compositions for this purpose 失效
    用于此目的的O-酰化苯酚衍生物和酰化组合物的方法

    公开(公告)号：US4315861A

    公开(公告)日：1982-02-16

    申请号：US246412

    申请日：1981-03-23

    申请人： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Istvan Turcsan ,  Istvan Jelinek ,  Eva Somfai ,  Laszlo Simandi

    发明人： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Istvan Turcsan ,  Istvan Jelinek ,  Eva Somfai ,  Laszlo Simandi

    IPC分类号： C07D307/86 ,  C07D317/10 ,  C07C125/067

    CPC分类号： C07D307/86

    摘要： A process is disclosed for preparing a carbamic acid phenyl ester of the formula (I) ##STR1## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, or aralkyl having 7 to 16 carbon atoms, wherein the aryl, cycloalkyl or aralkyl is unsubstituted or substituted by at least one alkyl group having 1 to 8 carbon atoms;R.sub.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, cyanomethyl, 1,3-dioxolan-2-yl, or carboalkoxyamino wherein the alkoxy group contains 1 to 4 carbon atoms;R.sub.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms; orR.sub.1 and R.sub.2 form together a carbocyclic ring or a heterocyclic ring fused to the phenyl ring wherein the carbocyclic ring of the heterocyclic ring is unsubstituted or substituted by at least one alkyl having 1 to 8 carbon atoms, which comprises acylating a phenol of the formula (II) ##STR2## with a compound of the formula (IV) ##STR3## in the presence of a base. The compounds obtained are valuable intermediates.

    摘要翻译： 公开了制备式（I）的氨基甲酸苯酯的方法，其中R是具有1至8个碳原子的烷基，具有5或6个碳原子的芳基，环烷基或具有7至16个碳原子的芳烷基， 其中芳基，环烷基或芳烷基是未取代的或被至少一个具有1至8个碳原子的烷基取代; R1是氢，具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基，氰基甲基，1,3-二氧戊环-2-基或烷氧基氨基，其中烷氧基含有1至4个碳原子; R2是氢，卤素，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基; 或者R 1和R 2一起形成稠合到苯环的碳环或杂环，其中杂环的碳环是未取代的或被至少一个具有1至8个碳原子的烷基取代，其包括酰化式 （II）的化合物与式（IV）的化合物在碱的存在下反应。 所得化合物是有价值的中间体。

    Process for O-acylating phenol derivatives and acylating compositions for this purpose
    3.
    发明授权
    Process for O-acylating phenol derivatives and acylating compositions for this purpose 失效
    用于此目的的O-酰化苯酚衍生物和酰化组合物的方法

    公开(公告)号：US4323469A

    公开(公告)日：1982-04-06

    申请号：US201508

    申请日：1980-10-28

    申请人： Gyorgy Lugosi ,  Antal S. May ,  Janos Bodnar ,  Istvan Turcsan ,  Istvan Jelinek ,  Eva Somfai ,  Laszlo Simandi

    发明人： Gyorgy Lugosi ,  Antal S. May ,  Janos Bodnar ,  Istvan Turcsan ,  Istvan Jelinek ,  Eva Somfai ,  Laszlo Simandi

    IPC分类号： C07D307/86 ,  C09K3/00

    CPC分类号： C07D307/86

    摘要： The invention relates to a process for the preparation of carbamic acid phenyl esters of the formula (I) ##STR1## by acylating phenol derivatives of the formula (II) ##STR2## wherein R is alkyl having 1 to 8 carbon atoms, aryl, cycloalkyl having 5 or 6 carbon atoms, aralkyl having 7 to 16 carbon atoms which groups can be substituted by one or more alkyl groups,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or acylamino,R.sup.2 is hydrogen, halogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms, or ifR.sup.1 and R.sup.2 represent alkyl and/or alkoxy, they can form together a carbocyclic ring.According to the invention the phenol derivatives of the general formula (II), wherein R.sup.1 and R.sup.2 are as defined above, are reacted with N-carbamoyl-saccharin derivatives of the formula (IV) ##STR3## wherein R has the same meaning as defined above, in the presence of a base.

    摘要翻译： 本发明涉及通过酰化式（II）的苯酚衍生物（II）制备式（I）的氨基甲酸苯酯的方法，其中R是具有1至8个碳原子的烷基 碳原子，芳基，具有5或6个碳原子的环烷基，具有7至16个碳原子的芳基，该基团可以被一个或多个烷基取代，R 1是氢，具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基 原子或酰氨基，R 2是氢，卤素，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基，或者如果R 1和R 2表示烷基和/或烷氧基，则它们可以一起形成碳环。 根据本发明，其中R 1和R 2如上定义的通式（II）的酚衍生物与式（Ⅳ）的N-氨基甲酰基 - 糖精衍生物反应其中R具有相同的 意义如上所述，在碱的存在下。

    Process for the preparation of non-pyrophoric palladium catalysts
    5.
    发明授权
    Process for the preparation of non-pyrophoric palladium catalysts 失效
    非自发钯催化剂的制备方法

    公开(公告)号：US4239653A

    公开(公告)日：1980-12-16

    申请号：US963882

    申请日：1978-11-27

    申请人： Janos Bodnar ,  Gyorgy Lugosi ,  Gyorgy L. Nagy

    发明人： Janos Bodnar ,  Gyorgy Lugosi ,  Gyorgy L. Nagy

    IPC分类号： B01J23/44 ,  B01J21/18

    CPC分类号： B01J23/44

    摘要： The present invention relates to a process for the preparation of non-pyrophoric catalyst having controlledparticle size and activity comprising suspending active charcoal of homogeneous pore distribution in a diluted solution of a palladium salt or salt complex, if desired in the presence of an aliphatic alcohol, stirring the solution, filtering the catalyst coal, followed by treatment of the sorbed palladium salt or salt complex with alkali if desired and stirring it as long as required for the accumulation of the sorbed palladium compounds, reducing same by methods known, repeating the above mentioned steps, if desired any number of times and drying the obtained catalyst after washing.

    摘要翻译： 本发明涉及一种制备具有受控粒径和活性的非发泡催化剂的方法，其包括在脂族醇存在下，将钯盐或盐络合物的稀溶液悬浮均匀孔分布的活性炭， 搅拌溶液，过滤催化剂煤，然后如果需要，用碱处理吸附的钯盐或盐络合物，并搅拌，只要吸附的钯化合物的积聚就可以，通过已知的方法将其还原，重复上述 步骤，如果需要任意次数，并在洗涤后干燥得到的催化剂。

    Process for the preparation of benzimidazole-thiol
    7.
    发明授权
    Process for the preparation of benzimidazole-thiol 失效
    苯并咪唑硫醇的制备方法

    公开(公告)号：US4675413A

    公开(公告)日：1987-06-23

    申请号：US811246

    申请日：1985-12-19

    申请人： Maria Bakonyi ,  Gyorgy Lugosi ,  Tamas Kallai ,  Maria Hima nee Toth ,  Tibor Montai ,  Maria Sziladi

    发明人： Maria Bakonyi ,  Gyorgy Lugosi ,  Tamas Kallai ,  Maria Hima nee Toth ,  Tibor Montai ,  Maria Sziladi

    IPC分类号： C07D235/32 ,  C07D235/04

    CPC分类号： C07D235/32

    摘要： A new process is disclosed for preparing a compound of the formula (I) ##STR1## wherein R is C.sub.1 to C.sub.5 alkyl; which comprises reducing a compound of the formula (II) ##STR2## or salt thereof wherein A is --SO.sub.2 X, --SOH, --SOA.sup.1, or --SA.sup.1 group,X is chlorine or hydrogen; andA.sup.1 is a group of the Formula ##STR3## with the aid of aluminum activated with a catalytic amount of a metal and/or metal salt in a mixture of water, a mineral acid, and an aliphatic carboxylic acid having 1 to 3 carbon atoms at a temperature of 0.degree. to 100.degree. C., thereafter, optionally, the product is recovered from an acid medium at a pH range of 2 to 3 in crystalline form.

    摘要翻译： 公开了用于制备式（I）化合物的新方法，其中R是C1至C5烷基; 其包括还原式（II）的化合物或其盐，其中A是-SO 2 X，-SOH，-SOA 1或-SA 1基团，X是氯或氢; 并且A1是通过在水，无机酸和具有1至3个碳原子的脂族羧酸的混合物中催化量的金属和/或金属盐活化的铝的助催化剂的组合的“IMAGE” 在0℃至100℃的温度下，然后，任选地，该产物从酸性介质中以2至3的结晶形式从pH值范围内回收。

    Process for the preparation of 6-demethyl-6-deoxy-6-methylene-5-oxytetracyclin and the 11A-chloro-derivative thereof
    10.
    发明授权
    Process for the preparation of 6-demethyl-6-deoxy-6-methylene-5-oxytetracyclin and the 11A-chloro-derivative thereof 失效
    6-脱甲基-6-脱氧-6-亚甲基-5-氧四环素及其11A-氯衍生物的制备方法

    公开(公告)号：US4659515A

    公开(公告)日：1987-04-21

    申请号：US646574

    申请日：1984-08-31

    申请人： Gyorgy Lugosi ,  Maria Hima nee Toth ,  Maria Bakonyi ,  Sandor Szoke

    发明人： Gyorgy Lugosi ,  Maria Hima nee Toth ,  Maria Bakonyi ,  Sandor Szoke

    IPC分类号： C07C231/00 ,  C07C67/00 ,  C07C231/12 ,  C07C233/00 ,  C07C237/26 ,  C07C309/73 ,  C07C103/19

    CPC分类号： C07C237/26 ,  C07C233/00 ,  C07C309/73

    摘要： The invention relates to a new and improved process for the preparation of 6-demethyl-6-deoxy-6-methylene-5-oxytetracycline and the 11a-chloro derivative thereof by dehydrating 11a-chloro-5-oxytetracycline-6,12-hemiketal, which comprises treating 11a-chloro-5-oxytetracycline-6,12-hemiketal or an acid salt thereof with a dehydrating mixture formed by the reaction of chloro sulfonic acid and formic acid and isolating the 11a-chloro-6-demethyl-6-deoxy-6-methylene-5-oxytetracycline and salt thus obtained and optionally dehalogenating the same by reaction with a reducing agent.The advantage of the process of the present invention is that it is simple, economical and suitable for industrial scale manufacture and provides a pure product of high quality by excellent yields.

    摘要翻译： 本发明涉及一种通过使11a-氯-5-氧四环素-6,12-半缩酮脱水制备6-脱甲基-6-脱氧-6-亚甲基-5-土霉素及其11a-氯衍生物的新方法和改进方法 其包括用与氯磺酸和甲酸的反应形成的脱水混合物处理11a-氯-5-土霉素-6,12-半缩酮或其酸盐，并将11a-氯-6-去甲基-6- 脱氧-6-亚甲基-5-土霉素和盐，并通过与还原剂反应任选地使其脱卤。 本发明方法的优点在于它简单，经济，适用于工业规模的制造，并通过优异的成品率提供高品质的纯净产品。