公开(公告)号：US5237095A

公开(公告)日：1993-08-17

申请号：US961801

申请日：1992-10-16

申请人： Jollie D. Godfrey, Jr. ,  Richard H. Mueller ,  Thomas P. Kissick ,  Janak Singh

发明人： Jollie D. Godfrey, Jr. ,  Richard H. Mueller ,  Thomas P. Kissick ,  Janak Singh

IPC分类号： C07B57/00 ,  C07C45/58 ,  C07C49/753 ,  C07C51/487 ,  C07C61/35 ,  C07C69/68 ,  C07C69/743 ,  C07C309/73 ,  C07D473/00

CPC分类号： C07D473/00 ,  C07B57/00 ,  C07C309/73 ,  C07C45/58 ,  C07C49/753 ,  C07C51/487 ,  C07C61/35 ,  C07C69/68 ,  C07C69/743 ,  C07C2101/04

摘要： Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.

公开(公告)号：US5233086A

公开(公告)日：1993-08-03

申请号：US961946

申请日：1992-10-16

申请人： Jollie D. Godfrey, Jr. ,  Richard H. Mueller ,  Thomas P. Kissick ,  Janak Singh

发明人： Jollie D. Godfrey, Jr. ,  Richard H. Mueller ,  Thomas P. Kissick ,  Janak Singh

IPC分类号： C07B57/00 ,  C07C45/58 ,  C07C49/753 ,  C07C51/487 ,  C07C61/35 ,  C07C69/68 ,  C07C69/743 ,  C07C309/73 ,  C07D473/00

CPC分类号： C07D473/00 ,  C07B57/00 ,  C07C309/73 ,  C07C45/58 ,  C07C49/753 ,  C07C51/487 ,  C07C61/35 ,  C07C69/68 ,  C07C69/743 ,  C07C2101/04

摘要： Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylene-cyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.

摘要翻译： 外消旋Feist酸用（R） - （+） - α-甲基苄胺处理，得到（1R-反式）-3-亚甲基 - 环丙烷-1,2-二羧酸，（R）-α-甲基苄胺（1:1） 盐。 然后将该盐转化为（1R-反式）-3-亚甲基-1,2-环丙烷二羧酸二甲酯，其是制备抗病毒剂[1R-（1α，2β，3α） ] -2-氨基-9- [2,3-双（羟甲基）环丁基] -1,9-二氢-6H-嘌呤-6-酮。 改进的方法还可以从分辨率中回收外消旋的Feist酸。

公开(公告)号：US5147645A

公开(公告)日：1992-09-15

申请号：US590690

申请日：1990-10-01

申请人： Bernd Wolf ,  Hans Theobald ,  Winfried Zombik ,  Norbert Goetz ,  Jochen Wild ,  Albrecht Harreus ,  Peter Hofmeister ,  Christoph Kuenast ,  Jacobus J. DeKramer

发明人： Bernd Wolf ,  Hans Theobald ,  Winfried Zombik ,  Norbert Goetz ,  Jochen Wild ,  Albrecht Harreus ,  Peter Hofmeister ,  Christoph Kuenast ,  Jacobus J. DeKramer

IPC分类号： C07D207/325 ,  A01N43/36 ,  A01N53/00 ,  A01N53/06 ,  C07C33/20 ,  C07C33/30 ,  C07C33/46 ,  C07C33/50 ,  C07C69/007 ,  C07C69/65 ,  C07C69/734 ,  C07C69/743 ,  C07C69/747 ,  C07C229/18 ,  C07C255/36 ,  C07C255/41 ,  C07D207/32 ,  C07D207/337

CPC分类号： C07D207/337 ,  A01N43/36 ,  A01N53/00 ,  C07C255/36 ,  C07C33/20 ,  C07C33/30

摘要： Benzyl esters of the formula I ##STR1## where R.sup.1 is methyl, ethyl, halogen, methoxy or ethoxy, R.sup.2 is alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, bicycloalkenyl, C.sub.1 -C.sub.5 -alkyl-substituted cycloalkyl, C.sub.1 -C.sub.5 -substituted cycloalkenyl, C.sub.1 -C.sub.5 -alkyl-substituted bicycloalkyl or C.sub.1 -C.sub.5 -alkyl-substituted bicycloalkenyl, R.sup.3 is hydrogen, cyano, C.sub.2 -C.sub.4 -alkynyl, C.sub.2 -C.sub.4 -alkenyl or C.sub.1 -C.sub.4 -alkyl, A is the carboxylate radical of an acid component typical for pyrethroids and X is hydrogen or halogen, with the proviso that R.sup.2 is not CH.sub.2 --CH.dbd.CH--B when B is hydrogen, alkyl or alkenyl and at the same time R.sup.1 is methyl or halogen, and furthermore with the proviso that R.sup.2 is not methyl when R.sup.1 is methyl, their manufacture, their use for combating pests, and precursors for manufacturing the benzyl esters.

摘要翻译： 式I的苄酯（I）其中R1是甲基，乙基，卤素，甲氧基或乙氧基，R2是烷基，烯基，环烷基，环烯基，双环烷基，双环烯基，C1-C5-烷基取代的环烷基，C1- C 5 - 取代的环烯基，C 1 -C 5 - 烷基取代的双环烷基或C 1 -C 5 - 烷基取代的双环烯基，R 3是氢，氰基，C 2 -C 4 - 炔基，C 2 -C 4 - 烯基或C 1 -C 4烷基，A是 典型的拟除虫菊酯的酸成分的羧酸酯基，X是氢或卤素，条件是当B是氢，烷基或烯基时，R2不是CH2-CH = CH-B，同时R1是甲基或卤素，以及 此外，条件是当R1是甲基时，R2不是甲基，它们的制备，它们用于防治害虫的用途和用于制备苄基酯的前体。

公开(公告)号：US5110976A

公开(公告)日：1992-05-05

申请号：US696580

申请日：1991-05-07

申请人： Gyorgy Hidasi ,  Istvan Szekely ,  Bela Bertok ,  Sandor Zoltan ,  Lajos Nagy ,  Antal Gajari ,  Eva Somfai ,  Agnes Hegedus ,  Laszlo Pap ,  Rudolf Soos ,  Erzsebet Radvany ,  Sandor Botar ,  Tamas Szabolcsi

发明人： Gyorgy Hidasi ,  Istvan Szekely ,  Bela Bertok ,  Sandor Zoltan ,  Lajos Nagy ,  Antal Gajari ,  Eva Somfai ,  Agnes Hegedus ,  Laszlo Pap ,  Rudolf Soos ,  Erzsebet Radvany ,  Sandor Botar ,  Tamas Szabolcsi

IPC分类号： C07C69/747 ,  A01N20060101 ,  A01N37/34 ,  A01N53/00 ,  A01N53/08 ,  A01P7/04 ,  C07B20060101 ,  C07B57/00 ,  C07B61/00 ,  C07B63/04 ,  C07C20060101 ,  C07C67/52 ,  C07C69/743 ,  C07C253/30 ,  C07C253/34 ,  C07C255/00 ,  C07C255/37 ,  C07C255/39

CPC分类号： A01N53/00

摘要： A process is disclosed for preparing a synergistic, crystalline product consisting of solely enantiomer pair 1RCisS and 1SCisR and enantiomer pair 1RTransS and 1STransR of cypermethrin in a 3:7 to 5:5 crystalline mixture, which comprises the steps of: (a) epimerizing an oily melt or a saturated solution of enantiomer pair 1RCisS and 1SCisR and enantiomer pair 1RTransS and 1STransR in a ratio other than 3:7 to 5:5, or a mixture of enantiomer pair 1RCisS and 1SCisR, enantiomer pair 1RTransS and 1STransR together with enantiomer pair 1RCisR and 1SCisS and enantiomer pair 1RTransR and 1STransS, said saturated solution including a protic or apolar, aprotic inert organic solvent by treating said oily melt or saturated solution with an organic or inorganic base at a temperature of -15.degree. C. to 30.degree. C. to precipitate crystals consisting solely of the 1RCisS and 1SCisR and the 1RTransS and 1RTransR enantiomer pairs in a 3:7 to 5:5 weight ratio; (b) isolating the precipitated crystals consisting solely of the enantiomer pairs 1RCisS and 1SCisR and 1RTransS and 1STransR at -10.degree. to 30.degree. C., optionally after inoculating the reaction mixture with a seeding crystal consisting of a mixture of the enantiomer pairs 1RCisS and 1SCisR and 1RTransS and 1STransR at a weight ratio of 3:7 to 5:5 before crystallization; and (c) repeating any of the above steps, if necessary.

公开(公告)号：US5089511A

公开(公告)日：1992-02-18

申请号：US467040

申请日：1990-01-18

申请人： Werner Bonin ,  Jean-Pierre Demoute ,  Jean Tessier

发明人： Werner Bonin ,  Jean-Pierre Demoute ,  Jean Tessier

IPC分类号： C07D209/48 ,  A01N53/00 ,  A01N53/02 ,  A23K1/16 ,  B01J27/122 ,  C07B37/04 ,  C07B61/00 ,  C07C67/343 ,  C07C69/743 ,  C07C235/06 ,  C07C253/30 ,  C07C255/37 ,  C07C255/39 ,  C07C327/44 ,  C07D213/64 ,  C07D213/647 ,  C07D213/68 ,  C07D233/72 ,  C07D307/45 ,  C07D309/38 ,  C07F7/18

CPC分类号： C07D213/647 ,  A01N53/00 ,  A23K20/00

摘要： A process for the preparation of trifluoromethylvinyl compounds in all their possible steroisomeric forms and mixtures thereof comprising reacting a salt of trifluoroacetic acid with a halovinyl compound in the presence of a cuprous salt to obtain the same stero-specific compound and all possible stero-isomeric forms and mixtures thereof of 1R, trans compounds of the formula ##STR1## wherein R is an alcohol residue used in pyrethrinoid series, or an alcohol residue capable of blocking the acid function, and Z is aryl or haloaryl and the double bond has Z geometry having pesticide activity.

公开(公告)号：US5066673A

公开(公告)日：1991-11-19

申请号：US482890

申请日：1990-02-22

申请人： Winfried Zombik ,  Hans Theobald ,  Bernd Wolf ,  Ludwig Schuster ,  Peter Hofmeister ,  Christoph Kuenast

发明人： Winfried Zombik ,  Hans Theobald ,  Bernd Wolf ,  Ludwig Schuster ,  Peter Hofmeister ,  Christoph Kuenast

IPC分类号： C07C69/743 ,  A01N53/00 ,  A01N53/06 ,  C07C67/00 ,  C07C69/753 ,  C07C255/39

CPC分类号： A01N53/00

摘要： Substituted benzyl 2-phenylalk(en)-1-ylcyclopropanecarboxylates of the general formula I ##STR1## where R.sup.1 is halogen or in each case low molecular weight, alkyl, alkoxy, haloalkyl or haloalkoxy (n=1 to 5),R.sup.2 is halogen or, in each case low molecular weight, alkyl or haloalkyl,R.sup.3, R.sup.4 are halogen or each is an electron in a double bond formed by them together,R.sup.5 is hydrogen or, in each case low molecular weight, alkyl, alkenyl, alkynyl or cyano,R.sup.6 is halogen or alkyl (n=1 to 4),R.sup.7 is halogen (p=0 to 25),and their use for combating pests.

摘要翻译： 烷基，烷氧基，卤代烷基或卤代烷氧基（n = 1-5），其中R 1是卤素，或者在各种情况下都是低分子量的取代的通式I（I）的2-苯基（en）-1-基环丙烷羧酸苄酯， R 2是卤素，或者在各种情况下都是低分子量的烷基或卤代烷基，R 3，R 4是卤素，或者各自是由它们一起形成的双键中的电子，R 5是氢或在各种情况下都是低分子量的烷基，烯基 ，炔基或氰基，R6是卤素或烷基（n = 1-4），R7是卤素（p = 0-25））及其用于防治害虫的用途。

公开(公告)号：US5004822A

公开(公告)日：1991-04-02

申请号：US16289

申请日：1987-02-19

申请人： Michael Elliott ,  Norman F. Janes ,  David A. Pulman

发明人： Michael Elliott ,  Norman F. Janes ,  David A. Pulman

IPC分类号： C07C69/747 ,  A01N37/08 ,  A01N53/00 ,  A01N53/02 ,  A01N53/04 ,  A01N53/06 ,  A01N53/08 ,  A01P7/04 ,  A61K31/215 ,  C07C45/29 ,  C07C47/546 ,  C07C47/575 ,  C07C61/40 ,  C07C67/00 ,  C07C69/743 ,  C07C253/00 ,  C07C255/39 ,  C07C255/40 ,  C07C255/53 ,  C07D209/48 ,  C07D209/49 ,  C07D307/36 ,  C07D307/42 ,  C07D307/45 ,  C07D307/46 ,  C07D307/54 ,  C07F1/10 ,  C07F9/50 ,  C07F9/535

CPC分类号： C07D209/48 ,  A01N53/00 ,  C07C255/00 ,  C07C45/29 ,  C07C45/292 ,  C07C47/546 ,  C07C47/575 ,  C07D209/49 ,  C07D307/42 ,  C07D307/46 ,  C07D307/54 ,  C07F9/5352

摘要： New insecticides are of formula: ##STR1## wherein R.sup.1 represents hydrogen or a methyl group; R.sup.2 represents hydrogen or a halogeno or lower alkyl group; R.sup.3 represents hydrogen or a halogen, lower alkyl (which is difference to R.sup.2 when R.sup.2 represents a lower alkyl group) or carboloweralkoxy group which contains at least 2 carbon atoms in the lower alkoxy residue when R.sup.2 represents methyl or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent a cycloalkylene ring having at least one endocyclic carbon to carbon double bond; with the proviso that (a) R.sup.2 and R.sup.3 each represent hydrogen only when R.sup.1 represents methyl and (b) R.sup.3 contains at least 2 carbon atoms when R.sup.1 and R.sup.2 each represent hydrogen; and R represents a group which form insecticidal esters with chrysanthemic acid e.g. 5-benzyl-3-furylmethyl, 3-phenoxybenzyl, .alpha.-cyano-3-phenoxybenzyl. The esters are prepared by forming the ester linkage conventionally or by a Wittig reaction using a 3-formyl- or 3-acetyl-2,2-dimethyl cyclopropane carboxylic acid esterified with the desired residue or by an alkyl group which is subsequently converted to the desired residue.

摘要翻译： 新的杀虫剂具有下式：其中R 1表示氢或甲基; R2表示氢或卤代或低级烷基; R3表示氢或卤素，低级烷基（当R2表示低级烷基时与R2不同）或当R2表示甲基或R2和R3与碳时在低级烷氧基残基中含有至少2个碳原子的羧基烷氧基 它们所连接的原子表示具有至少一个内环碳 - 碳双键的亚环烷基环; 条件是（a）当R1表示甲基时，R2和R3各自表示氢，（b）当R 1和R 2各自表示氢时，R 3含有至少2个碳原子; R表示与菊酸形成杀虫酯的基团。 5-苄基-3-呋喃基甲基，3-苯氧基苄基，α-氰基-3-苯氧基苄基。 酯通过常规形成酯键或通过Wittig反应制备，使用用所需残基酯化的3-甲酰基或3-乙酰基-2,2-二甲基环丙烷羧酸或通过烷基将其转化为 所需残留物。

公开(公告)号：US4999451A

公开(公告)日：1991-03-12

申请号：US343318

申请日：1989-04-26

申请人： Kiyoshi Kondo ,  Kiyohide Matsui ,  Akira Negishi ,  Yuriko Takahatakae

发明人： Kiyoshi Kondo ,  Kiyohide Matsui ,  Akira Negishi ,  Yuriko Takahatakae

IPC分类号： A01N53/08 ,  C07C43/14 ,  C07C43/32 ,  C07C69/533 ,  C07C69/65 ,  C07C69/74 ,  C07C69/743

CPC分类号： C07C43/32 ,  C07C43/14 ,  C07C67/00 ,  C07C67/03 ,  C07C67/27 ,  C07C67/317 ,  C07C67/343 ,  C07C2101/02

摘要： Novel synthesis of dihalovinylcyclopropanecarboxylates, including potent insecticides, are described. The processes begin with the reaction between an alkenol and an orthoester to produce a .gamma.-unsaturated carboxylate, followed by the catalyzed addition of a carbon tetrahalide to the double bond and dehydrohalogenation to produce a cyclopropane derivative.

公开(公告)号：US4960922A

公开(公告)日：1990-10-02

申请号：US32365289

申请日：1989-03-15

申请人： FMC CORP

发明人： HOARE JOHN H

IPC分类号： C07C69/743

CPC分类号： C07C69/743

摘要： Esters of cis or trans-3[2-(E/Z)-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethlcyclopro panecarboxylic acid, or mixtures thereof, which are useful as insecticides or as intermediaes of pyrethroid insecticides may be prepared by the dehydrohalogenation of corresponding esters of cis/trans-3(2,2-dichloro-3,3,3-trifluoropropyl)-2,2-dimethylcyclopropa necarb oxylic acid with a catalytic amount of a cyclic amidine in the presence of a stoichiometric amount of an alkali metal or alkaline earth metal base, or combinations thereof and a polar aprotic solvent. The use of cyclic amidines as dehydrohalogenation catalysts permits reactions to be carried out at lower temperatures, shorter reaction times, and with reduced unwanted by-products compared with prior art methods using metal bases alone.

摘要翻译： 顺式或反式-3 [2-（E / Z） - 氯-3,3,3-三氟-1-丙烯基）-2,2-二甲基环戊烷羧酸或其混合物的酯可用作杀虫剂或作为 拟除虫菊酯类杀虫剂的中间体可以通过顺式/反式-3（2,2-二氯-3,3,3-三氟丙基）-2,2-二甲基环丙烷氧基酸的相应酯的脱卤化氢与催化量的环状 脒在化学计量量的碱金属或碱土金属碱的存在下，或其组合和极性非质子溶剂。 使用环状脒作为脱卤化氢催化剂，与使用单独使用金属碱的现有技术方法相比，可以在较低温度下进行反应，缩短反应时间，减少不需要的副产物。

公开(公告)号：US4845126A

公开(公告)日：1989-07-04

申请号：US916546

申请日：1986-09-16

申请人： Gyorgy Hidasi ,  Istvan Szekely ,  Bela Bertok ,  Sandor Zoltan ,  Lajos Nagy ,  Antal Gajari ,  Eva Somfai ,  Agnes Hegedus ,  Laszlo Pap ,  Rudolf Soos ,  Erzsebet Radvany ,  Sandor Botar ,  Tamas Szabolcsi

发明人： Gyorgy Hidasi ,  Istvan Szekely ,  Bela Bertok ,  Sandor Zoltan ,  Lajos Nagy ,  Antal Gajari ,  Eva Somfai ,  Agnes Hegedus ,  Laszlo Pap ,  Rudolf Soos ,  Erzsebet Radvany ,  Sandor Botar ,  Tamas Szabolcsi

IPC分类号： C07C69/747 ,  A01N20060101 ,  A01N37/34 ,  A01N53/00 ,  A01N53/08 ,  A01P7/04 ,  C07B20060101 ,  C07B57/00 ,  C07B61/00 ,  C07B63/04 ,  C07C20060101 ,  C07C67/52 ,  C07C69/743 ,  C07C253/30 ,  C07C253/34 ,  C07C255/00 ,  C07C255/37 ,  C07C255/39

CPC分类号： A01N53/00

摘要： According to the present invention there is provided 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 pyrethroid of the Formula /I/ ##STR1## namely substantially only the 1RtransS and 1StransR entantiomer-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, stabilizing agents, wetting agents, emulsifying agents, dispersing agents, antifoam agents, dileunts 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.

摘要翻译： PCT No.PCT / HU86 / 00004 Sec。 371日期1986年10月15日第 102（e）1986年10月15日日期PCT提交1986年1月16日PCT公布。 第WO86 / 04216号公报 日本1986年7月31日。根据本发明，提供了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，其特征在于包含0.001至99重量％的式（I）的合成拟除虫菊酯 （I）即基本上只有可能的八个异构体中的1RtransS和1StransR对映异构体对/ Ib /出，任选地与至多100重量％的一种或多种活化剂/ 和助剂，特别是抗氧化剂，稳定剂，润湿剂，乳化剂，分散剂，消泡剂，二酸酐和/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它对温血动物和有用寄生虫的毒性较小，因此对环境的危害小得多。