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    PROCESS FOR THE PREPARATION OF BENZYL-ETHERS
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF BENZYL-ETHERS 审中-公开
    制备苯甲醚的方法

    公开(公告)号：WO1998022416A1

    公开(公告)日：1998-05-28

    申请号：PCT/HU1997000073

    申请日：1997-11-12

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT. ,  ARVAI, Géza ,  BERTOK, Béla ,  KURUCZNÉ RIBAI, Zsuzsanna ,  PAP, László ,  SZÉKELY, István

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT.

    IPC: C07C41/09

    CPC classification number: C07D317/54 ,  C07C41/09 ,  C07C43/23 ,  C07C43/215 ,  C07C43/225 ,  C07C43/166

    Abstract: The subject of the invention is the process for the preparation of mixed ethers of general formula (I), wherein Ar represents an alicyclic, aromatic or one or more heteroatom-containing heterocyclic moiety, optionally substituted by one or more C1-4 alkoxy, methylenedioxy, C1-4 alkyl, halogen, C1-4 haloalkyl or nitro-group, and/or condensed with a benzine ring, R and R independently mean hydrogen C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, phenyl, substituted phenyl, C3-6 cycloalkyl group, R means C1-6 alkyl, C3-6 alkenyl, or C3-6 alkynyl group, optionally substituted by one or more C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl, C1-6 haloalkyl group, or halogen atom; or a C1-4 alkyloxy-C1-4 alkyloxy-C1-4 alkyl group characterized by, that the compounds of general formula (II), wherein X means hydroxy, halogen or sulphonester leaving group, are reacted in the presence of acid, Lewis acid, metal oxide or metal carbonate, with 1-3 molar equivalent of the alcohol of general formula (III), wherein the meaning of the substituent is as defined above, the resulting ether of general formula (I) is isolated, if desired, stabilized by the addition of a base and/or an anti-oxidant, and if desired the excess of the alcohol is recovered.

    Abstract translation: 本发明的主题是制备通式（I）的混合醚的方法，其中Ar表示脂环族，芳族或一个或多个含杂原子的杂环部分，任选被一个或多个C 1-4烷氧基亚甲二氧基 ，C 1-4烷基，卤素，C 1-4卤代烷基或硝基，和/或与苯环稠合，R 1和R 2独立地表示氢，C 1-4烷基，C 1-4卤代烷基， 4烯基，苯基，取代的苯基，C 3-6环烷基，R 3表示任选被一个或多个C 1-6烷基，C 3-6的C 1-6烷基，C 3-6烯基或C 3-6炔基取代 烯基，C 3-6炔基，C 1-6卤代烷基或卤素原子; 或C 1-4烷氧基-C 1-4烷氧基-C 1-4烷基，其特征在于，其中X表示羟基，卤素或磺基取代基的通式（II）化合物在酸存在下反应，路易斯 酸，金属氧化物或金属碳酸盐，与1-3摩尔当量的通式（III）的醇反应，其中取代基的含义如上所定义，如果需要，所得的通式（I）的醚是分离的， 通过加入碱和/或抗氧化剂来稳定，如果需要，回收过量的醇。

    PROCESS FOR THE PREPARATION OF BENZYL-ETHERS BY USE OF PHASE TRANSFER
    3.
    发明申请
    PROCESS FOR THE PREPARATION OF BENZYL-ETHERS BY USE OF PHASE TRANSFER 审中-公开
    通过使用相转移制备苯甲醚的方法

    公开(公告)号：WO1998022417A1

    公开(公告)日：1998-05-28

    申请号：PCT/HU1997000074

    申请日：1997-11-12

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT. ,  ARVAI, Géza ,  BERTOK, Béla ,  KURUCZNÉ RIBAI, Zsuzsanna ,  PAP, László ,  SZÉKELY, István

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT.

    IPC: C07C41/16

    CPC classification number: C07C41/16 ,  C07D317/54 ,  C07C43/215 ,  C07C43/225 ,  C07C43/2055

    Abstract: The subject of the invention is the process for the preparation of mixed ethers of general formula (I), wherein Ar represents an alicyclic, aromatic or one or more heteroatom-containing heterocyclic moiety, optionally substituted by one or more C1-4 alkoxy, methylenedioxy, C1-4alkyl, halogen, C1-4haloalkyl or nitro-group, and/or condensed with a benzene ring; R means hydrogen, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, phenyl, substituted phenyl, C3-6cycloalkyl group; R means C1-6alkyl, C3-6alkenyl, or C3-6alkinyl group, optionally mono- or poly-substituted by C1-6alkyl, C1-6alkoxy, C3-6alkenyl, C3-6alkinyl, C1-6haloalkyl group or by halogen atom; or a C1-4 alkyloxy-C1-4alkyl-oxy-C1-4alkyl group. n = 1,2 by the reaction of compounds of general formula (II), wherein R and n have the same meaning as above; X means hydroxy, halogen or sulfonester leaving group, with the compounds of the general formula (III): R2-Y, wherein R has the same meaning as above; Y means hydroxy, halogen or sulfonester leaving group, with the proviso that one of the reaction partners of general formulae (II) and (III) is an alcohol, characterized by, that the reaction is performed under heterogenous conditions in presence of an aqueous base and a phase transfer catalyst, and the resulting product is optionally stabilized by the addition of a base and/or anti-oxidant.

    Abstract translation: 本发明的主题是制备通式（I）的混合醚的方法，其中Ar表示脂环族，芳族或一个或多个含杂原子的杂环部分，任选被一个或多个C 1-4烷氧基亚甲二氧基 ，C 1-4烷基，卤素，C 1-4卤代烷基或硝基，和/或与苯环稠合; R 1表示氢，C 1-4烷基，C 1-4卤代烷基，C 2-4烯基，苯基，取代的苯基，C 3-6环烷基; R 2表示C 1-6烷基，C 3-6烯基或C 3-6炔基，任选被C 1-6烷基，C 1-6烷氧基，C 3-6烯基，C 3-6烯基，C 1-6卤代烷基或卤素单取代或多取代 原子; 或C 1-4烷氧基-C 1-4烷基 - 氧基-C 1-4烷基。 通过通式（II）的化合物（其中R 1和n具有与上述相同的含义）的反应，n = 1,2; X表示羟基，卤素或砜类离去基团，与通式（III）的化合物：R2-Y，其中R 2具有与上述相同的含义; Y表示羟基，卤素或砜类离去基团，条件是通式（II）和（III）的反应伴侣之一是醇，其特征在于反应在异质条件下在碱水溶液 和相转移催化剂，并且所得产物任选地通过加入碱和/或抗氧化剂来稳定。

    IMPROVED PROCESS FOR THE PREPARATION OF AMIDOXIME DERIVATIVES
    4.
    发明申请
    IMPROVED PROCESS FOR THE PREPARATION OF AMIDOXIME DERIVATIVES 审中-公开
    改进酰胺衍生物的制备方法

    公开(公告)号：WO1990008131A1

    公开(公告)日：1990-07-26

    申请号：PCT/HU1990000003

    申请日：1990-01-10

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT ,  BERTOK, Béla ,  SZÉKELY, István ,  THURNER, Angelika ,  SOMFAI, Éva ,  BOTAR, Sándor ,  GAJARY, Antal ,  TAKACS, Kálmán ,  NAGY, Lajos

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT

    IPC: C07C251/58

    CPC classification number: C07D213/78 ,  C07C259/12 ,  C07D295/088

    Abstract: The invention relates to an improved process for preparing amidoxime derivatives of general formula (I), wherein R means a C2-15 group, which may be unsaturated and/or cyclic alkyl, aralkyl group or optionally substituted and/or condensed aromatic and/or heteroaromatic group; R stands for hydrogen or an optionally substituted straight or branched chain or cyclic and/or unsaturated C1-7 alkyl or aromatic group; R represents an optionally substituted straight or branched chain or cylic and/or unsaturated C1-7 alkyl or aromatic group; or R and R together with the adjacent nitrogen atom may form a 5- to 8-membered ring optionally containing other heteroatom(s); and X stands for halogen and their salts by reacting an amidoxime of general formula (II), wherein R is as defined above, in the presence of an alkaline substance, transforming the product to a salt with an acid or transforming the salt to the base, which comprises reacting the amidoxime with an alkaline metal hydroxide or alkaline metal alkoxide and dimethylformamide or 1,3-dimethyl-2-imidazolidinone, preferably in the presence of a proton source, reacting the amidoxime complex thus obtained preferably without isolation with an amine of general formula (III). The invention relates further to pure O-(2-hydroxy-piperidino-1-propil)nicotinic acid amidoxime hydrochloride and hydrobromide and O-(2-hydroxy-3-piperidino-1-propyl)nicotinic acid amidoxime base.

    Abstract translation: 本发明涉及一种制备通式（I）的偕胺肟衍生物的改进方法，其中R 1表示C2-15基团，其可以是不饱和和/或环状烷基，芳烷基或任选取代的和/或稠合的芳族 和/或杂芳族基团; R 2代表氢或任选取代的直链或支链或环状和/或不饱和的C 1-7烷基或芳基; R 3表示任选取代的直链或支链或环状和/或不饱和的C 1-7烷基或芳基; 或R 2和R 3与相邻的氮原子一起可以形成任选含有其它杂原子的5-至8-元环; X代表卤素及其盐，通过在碱存在下使通式（II）的偕胺肟（其中R 1如上述定义）在酸存在下反应，将产物转化为酸或转化盐 包括使偕胺肟与碱金属氢氧化物或碱金属醇盐和二甲基甲酰胺或1,3-二甲基-2-咪唑啉酮反应，优选在质子源存在下，使得到的偕胺肟配合物优选不与其分离而与 通式（III）的胺。 本发明还涉及纯O-（2-羟基 - 哌啶子基-1-丙基）烟酸偕胺肟盐酸盐和氢溴酸盐和O-（2-羟基-3-哌啶子基-1-丙基）烟酸偕胺肟碱。

    2,3,4-TRINOR-1,5-INTER-M-PHENYLENE-PROSTACYCLINE-I2 ANALOGUES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    5.
    发明申请
    2,3,4-TRINOR-1,5-INTER-M-PHENYLENE-PROSTACYCLINE-I2 ANALOGUES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 审中-公开
    2,3,4-三硝基-1,5-间 - 间苯二酚 - 前列环素-12类似物，其制备方法和含有其的药物组合物

    公开(公告)号：WO1983004021A1

    公开(公告)日：1983-11-24

    申请号：PCT/HU1983000021

    申请日：1983-05-06

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA ... ,  SZÉKELY, István ,  LOVASZ, Marianna ,  BOTAR, Sándor ,  DOLGOSNÉ KÉKESI, Krisztina ,  BERTOK, Béla ,  GAJARY, Antal ,  SZABOLCSI, Tamás ,  KOVACS, Gábor

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA ...

    IPC: C07C177/00

    CPC classification number: C07D257/04 ,  C07C65/03 ,  C07C65/21 ,  C07C205/58 ,  C07C255/00 ,  C07C405/00 ,  C07C405/0041 ,  C07C405/0083 ,  C07D307/935 ,  C07D307/937 ,  C07D405/10 ,  C07F9/4015 ,  C07F9/5352 ,  C07F9/5456

    Abstract: New 2,3,4-trinor-1,5-inter-m-phenylene-PGI2 derivatives (wherein A stands for carboxy, cyano, tetrazolyl or -COOR or -CONR R ; R is C1-4 alkyl or an equivalent of a pharmacologically acceptable cation: R and R each stands for hydrogen, phenyl; C1-5 alkyl, optionally substituted by carboxy, hydroxy, phenyl or C2-5 alkoxycarbonyl; or C1-4 alkyl-sulfonyl; or R and R together form an alpha , omega -alkylene chain containing 3-6 carbon atoms; B stands for oxygen or methylene; Y is optionally bromo-substituted vinylene or a -C=C- group: R stands for hydrogen or tetrahydro-pyran-2-yl; R represents an alkyl group containing 5-9 carbon atoms, which can be optionally interrupted by one or more oxygen atom(s) or -CH=CH- or -C=C- group(s) and/or optionally substituted by halogen; or a phenoxymethyl group optionally substituted by halogen or trifluoromethyl; or an alkenyloxymethyl group containing 3-5 carbon atoms; R is hydrogen or C1-4 alkyl; R stands for hydrogen, halogen, cyano, C1-4 alkyl or C1-4 alkoxy; R is hydrogen, halogen, cyano, nitro, hydroxy or C2-5 alkanoylamido; with the proviso that if R stands for an alkyl group containing 5-9 carbon atoms which is unsubstituted or not interrupted by an oxygen atom or a -CH=CH- or -C=C- group; or a phenoxymethyl group optionally substituted by halogen or trifluoromethyl, then either R or R is other than hydrogen, or A is other than carboxy or -COOR ) and a process for the preparation thereof. The new compounds of the general Formula I exhibit prolonged cytoprotecting and aggregation inhibiting and a low hypotensive effect and are superior to prostacycline in the prolonged duration of their activity.

    Abstract translation: 新的2,3,4-三硝基-1,5-间 - 间 - 亚苯基-PGI 2衍生物（其中A代表羧基，氰基，四唑基或-COOR 3或-CONR 1 R 2; R 3是C 1-4烷基或等同的药学上可接受的阳离子：R 1和R 2各自代表氢，苯基;任选被羧基，羟基，苯基或C 2-5烷氧基羰基取代的C 1-5烷基 ;或C 1-4烷基磺酰基;或R 1和R 2一起形成含有3-6个碳原子的α，ω-亚烷基链; B代表氧或亚甲基; Y任选为溴代亚乙烯基或 一个-C = C-基团：R 4代表氢或四氢 - 吡喃-2-基; R 5表示含有5-9个碳原子的烷基，其可以任选地被一个或多个氧原子中断 或-CH = CH-或-C = C-基团和/或任选被卤素取代;或任选被卤素或三氟甲基取代的苯氧基甲基;或含有3-5个碳原子的烯氧基甲基; R <6>是氢或C 1-4烷基; R 7代表氢 ，卤素，氰基，C 1-4烷基或C 1-4烷氧基; R 8是氢，卤素，氰基，硝基，羟基或C 2-5烷酰基氨基; 条件是如果R 5代表未被取代或未被氧原子或-CH = CH-或-C = C-基团中断的含有5-9个碳原子的烷基; 或任选被卤素或三氟甲基取代的苯氧基甲基，然后R 7或R 8不是氢，或A不是羧基或-COOR 3），以及其制备方法。 通式I的新化合物表现出延长的细胞保护和聚集抑制和低降血压作用，并且在其活性持续时间内优于前列环素。

    ARTHROPODICIDES AND PROCESS FOR THEIR PREPARATION
    6.
    发明申请
    ARTHROPODICIDES AND PROCESS FOR THEIR PREPARATION 审中-公开
    抗坏血酸及其制备方法

    公开(公告)号：WO1998018329A1

    公开(公告)日：1998-05-07

    申请号：PCT/HU1997000071

    申请日：1997-10-30

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT. ,  ARVAI, Géza ,  BERTOK, Béla ,  BLEICHER, Edit ,  CSIZ, László ,  CZUDOR, Irén ,  HEGEDÜS, Agnes ,  PAP, László ,  SZÉKELY, István

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA RT.

    IPC: A01N53/00

    CPC classification number: C07C67/14 ,  A01N53/00 ,  C07C69/743

    Abstract: The invention relates to an arthropodicidal ectoparasiticidal composition, characterized in that, it contains one or more representative(s) of 1S-trans, (1S-trans) alpha S or (1S-trans) alpha (R, S) isomers or a racemic (1S-trans) alpha S(1R-trans) alpha R isomer mixtrure of one or more cyclopropan carboxylic acid ester type compound(s) containing two asymmetric centers in the cyclopropane ring and optionally one or more further asymmetric center(s) in other part of the molecule in an amount of from 0,001-99 % by weight optionally in admixture with an amount of up to 100 % by weight of one or more auxiliary agent(s) particularly antioxidants, stabilising agents, wetting agents, emulsifying agents, dispersing agents, antifoam agents, diluents and/or fillers.

    Abstract translation: 本发明涉及一种节肢针刺杀螨杀虫剂组合物，其特征在于其含有一个或多个代表性的1S-反式，（1S-反式）αS或（1S-反式）α（R，S）异构体或外消旋 在环丙烷环中含有两个不对称中心的一种或多种环丙烷羧酸酯型化合物的（1S-反式）αS（1R-反式）αR异构体混合物和任选的一种或多种其它不对称中心 0.001-99重量％的一部分分子，任选地与至多100重量％的一种或多种助剂，特别是抗氧化剂，稳定剂，润湿剂，乳化剂，分散剂 试剂，消泡剂，稀释剂和/或填料。

    INSECTICIDAL COMPOSITION COMPRISING MORE THAN ONE ACTIVE INGREDIENTS
    8.
    发明申请
    INSECTICIDAL COMPOSITION COMPRISING MORE THAN ONE ACTIVE INGREDIENTS 审中-公开
    包含超过一个活性成分的杀虫剂组合物

    公开(公告)号：WO1986004216A1

    公开(公告)日：1986-07-31

    申请号：PCT/HU1986000004

    申请日：1986-01-16

    Applicant: CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA ... ,  HIDASI, György ,  SZÉKELY, István ,  BERTOK, Béla ,  ZOLTAN, Sándor ,  NAGY, Lajos ,  GAJARI, Antal ,  SOMFAI, Éva ,  HEGEDÜS, Agnes ,  PAP, László ,  SOOS, Rudolf ,  RADVANY, Erzsébet ,  BOTAR, Sándor ,  SZABOLCSI, Tamás

    Inventor： CHINOIN GYOGYSZER ÉS VEGYÉSZETI TERMÉKEK GYARA ...

    IPC: A01N53/00

    CPC classification number: A01N53/00 ,  A01N2300/00

    Abstract: A synergistic insecticidal composition containing more than one active ingredients and being harmless to environment characterized by comprising in an amount of from 0.001 to 99% by weight a synthetic pyrethroide of the formula (I) - namely substantially only the 1RtransS and 1StransR enantiomer-pair (Ib) out from the possible eight isomers - optionally in admixture with an amount of up to 100% by weight of one or more activator(s) and auxiliary agent(s), particularly antioxidants, stabilising agents, wetting agents, emulsifying agents, dispersing agents, antifoam agents, diluents and/or fillers. The enantiomer-pair Ib consisting of the 1RtransS and 1StransR isomers is new and the invention also relates to the said new enantiomer-pair and a process for the preparation thereof. The advantage of the insecticidal composition of the present invention is that it is less toxical towards warm-blooded animals and useful parasites and is therefore much less harmful to the environment.

    Abstract translation: 一种含有多于一种活性成分并且对环境无害的协同杀虫组合物，其特征在于其含量为0.001至99重量％的式（I）的合成拟除虫菊酯，即基本上仅为1RtransS和1StransR对映异构体对（ Ib）可能的八种异构体 - 任选地与至多100重量％的一种或多种活化剂和辅助剂，特别是抗氧化剂，稳定剂，润湿剂，乳化剂，分散剂 试剂，消泡剂，稀释剂和/或填料。 由1RtransS和1StransR异构体组成的对映体对1b是新的，本发明还涉及所述新的对映异构体对及其制备方法。 本发明的杀虫组合物的优点在于对温血动物和有用寄生虫的毒性较小，因此对环境的危害较小。

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