CAS: 55701-05-8; 3-(2,2-Dichlorovinyl)-2,2-Dimethylcyclopropane-1-Carboxylic Acid

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CAS号61976-24-7 2,2-dimethyl-3-... | CAS号52314-67-7 氯氰菊酰氯 | CAS号72345-89-2 6,6-dimethyl-4-... | CAS号7440-66-6 锌标准溶液 | CAS号59897-92-6 3.3-二甲基-4.6,6-三... | CAS号78548-59-1 ethyl (1R,3S)-3... | CAS号72183-78-9 2-(2',2'-dichlo... | CAS号61898-95-1 3-(2,2-二氯乙烯基)-2... | CAS号6124-79-4 4-甲基-2(5H)-呋喃酮 | CAS号52314-67-7 氯氰菊酰氯 | CAS号52315-07-8 氯氰菊酯 | CAS号53179-78-5 1R,3R-二溴菊酸 | CAS号67328-58-9 [3-(4-hydroxyph... | CAS号59609-49-3 二氯菊酸乙酯 | CAS号54407-47-5 氯烯炔菊酯

📜氯菊酯置于sodium Hydroxide体系中,用 甲醇,二氯甲烷 作为反应溶剂,化学反应 15.0H,以87.5%的收率获得产物二氯菊酸
参考文献:苄氯菊酯向鱼类中雌激素代谢产物的立体选择性生物转化
标题:苄氯菊酯向鱼类中雌激素代谢产物的立体选择性生物转化
摘要:这项研究调查了拟除虫菊酯杀虫剂氯菊酯(pm)的立体选择性生物转化及其所产生的雌激素活性.两者的结果在体内(雄性日本青鳉,在等离子体卵黄蛋白原(vtg)蛋白)和体外(初级虹鳟鱼肝细胞vtg-Mrna表达)检测表明pm的立体选择性雌激素活性.1个小号-顺观察-Pm具有显著更高的活性(p <=0.05)比1-[r-顺式对映体在两种体内和体外评估.pm的所有对映异构体均被氧化为4'-羟基pm(4Oh Pm)代谢物,并进行酯酶裂解为3-苯氧基苄醇(3-Pboh)和3-(4'-羟基苯氧基)-苄醇)(3,4'-Pboh).外消旋4Oh Pm以及3-Pboh,和3,4'-Pboh具有显著(p <=0.05)雌激素.1 S-Trans-Pm比相应的1 R-Trans-Pm进行了更广泛的酯酶裂解.酮康唑的抑制研究证实了所有立体异构体的细胞色素p450催化的羟基化以及pm的酯酶裂解.这些研究表明,由
DOI:10.1021/tx100167X

专利信息

专利号:US-4284582-A
优先权日:1978-04-28
标 题 :Process for the preparation of cyclopropane derivatives, intermediates in the synthesis of pyrethroid insecticides
发明人：KAYE ALBERT E; TUCKER ALAN C
权利人:ICI LTD
摘要:Compounds of formula: wherein both groups X are chlorine, bromine or trifluoromethyl, or one X is chlorine or bromine and the other is trifluoromethyl, and Y is -CN or -COOR in which R is an alkyl group, are obtained by (A) reacting a compound of the formula: wherein X1 is chlorine or bromine, with a compound of the formula: X2C=CH-CH=C(CH3)2 in the presence of metallic copper or at least one copper salt and a base, or (B) reacting a compound of the formula: Y-CH2-CN with a compound of the formula: X2C=CH-CH=C(CH3)2 and chlorine or bromine, in the presence of at least one reducible copper salt and a base, or (C) reacting a compound of formula: X-CH2-CN with a compound of the formula: wherein X1 is chlorine or bromine, in the presence of at least one copper salt. The compounds are intermediates in the synthesis of pyrethroid insecticides.

专利号:US-10647655-B2
优先权日:2016-09-02
标题:Method for the synthesis of permethrin
发明人：PULLAGURLA MANIK REDDY; NANDA KUMAR MECHERIL VALSAN; VELIGETLA MADHUSUDHANA RAO; RANGISETTY JAGADEESH BABU
权利人:BIOPHORE INDIA PHARMACEUTICALS PVT LTD
摘要:An improved method for the synthesis of substantially pure Permethrin having purity greater than 99.5% by Gas Chromatography provided. The embodiments also relates to a purification process of Permethrin by recrystallization from methanol-water mixture.

专利号:US-4328173-A
优先权日:1979-04-03
标题:Resolution of D,L-cis and D,L-trans 2,2-dimethyl-3-(2,2-dihalovinyl)-cyclopropane-1-carboxylic acids and salts thereof
发明人：JOLLY JEAN; GIGLIOTTI GIUSEPPE; PAVAN CHARLES; BULIDON JACQUES
权利人:ROUSSEL UCLAF
摘要:A novel process for the resolution of D,L-cis and D,L-trans 2,2-dimethyl-3-(2,2 -dihalovinyl)-cyclopropane-1-carboxylic acids of the formula ##STR1## wherein X is selected from the group consisting of fluorine, chlorine and bromine comprising salifying the said acid with an optically active base selected from the group consisting of D-ephedrine, L-ephedrine, D-N-methyl-ephedrine, L-N-methylephedrine, D-pseudo-ephedrine and L-pseudo-ephedrine to form the corresponding salt, recovering the said salt and subjecting the latter to acid hydrolysis to obtain the corresponding resolved acid which are intermediates for the synthesis of esters having a remarkable insecticidal activity.

专利号:US-4603218-A
优先权日:1983-06-03
标题 :Asymmetric synthesis of cyclopropanecarboxylate derivatives using chiral copper complex as catalyst
发明人：ARATANI TADATOSHI; YOSHIHARA HIROSHI; SUSUKAMO GOHFU
权利人:SUMITOMO CHEMICAL CO
摘要:A chiral copper complex which is produced by the reaction of a chiral copper complex of the formula: ##STR1## wherein R 1 is (a) alkyl group, or (b) aralkyl group; R 2 is (a) 2-alkoxyphenyl group, or (b) 2-alkoxy-5-alkylphenyl group; either one of X 1 and X 2 is (a) hydrogen atom, (b) halogen atom, (c) alkyl group, (d) alkoxy group, or (e) nitro group, or adjacent X 1 and X 2 together form a benzo group, with a mono-substituted hydrazine of the formula: n n R.sub.3 NHNH.sub.2 n n wherein R 3 is (a) aryl group, (b) aralkyl group, or (c) alkyl group. n The copper complex is used as a catalyst in the production of an optically active alkyl cyclopropanecarboxylate.

专利号:EP-0050534-B1
优先权日:1980-10-01
标题 :Esters of cyclopropane-carboxylic acids related to pyrethric acid, their preparation and use as insecticides
摘要:1. Claims (for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE) In all possible isomeric forms, or in the form of a mixture of isomers, the compounds with the formula I see diagramm : EP0050534,P45,F2 in which the cyclopropane acid copula is of 1R cis structure and the geometry of the double bond is E and in which R represents either a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing from 1 to 8 carbon atoms, possibly substituted by one or more functional groups, identical or different, or an aryl group containing from 6 to 14 carbon atoms, possibly substituted by one or more functional groups, identical or different, or a heterocyclic radical possibly substituted by one or more functional groups, identical or different, X represents a halogen atom and B represents either a benzyl radical possibly substituted by one or more radicals chosen from the group composed of alkyl radicals including from 1 to 4 carbon atoms, alkenyl radicals including from 2 to 6 carbon atoms, alkenyloxy radicals including from 2 to 6 carbon atoms, alkadienyl radicals including from 4 to 8 carbon atoms, the methylene dioxy radical and halogen atoms, or a see diagramm : EP0050534,P46,F1 group in which the substituent R1 represents a hydrogen atom or a methyl radical and the substituent R2 represents a monocyclic aryl or a -CH2 -C=-CH group and in particular a 5-benzyl-3-furyl methyl group, or a see diagramm : EP0050534,P46,F2 group in which a represents a hydrogen atom or a methyl radical and R3 represents an organic aliphatic radical including from 2 to 6 carbon atoms and one or more carbon-carbon unsaturations and in particular the -CH2 -CH=CH2 , -CH2 -CH=CH-CH3 , -CH2 -CH=CH-CH=CH2 , -CH2 -CH=CH-CH2 -CH3 radical, or a see diagramm : EP0050534,P46,F3 group, in which a represents a hydrogen atom or a methyl radical, R3 retains the same significance as before, each of R'1 and R'2 , identical or different, represents a hydrogen atom, a halogen atom, an alkyl radical including from 1 to 6 carbon atoms, an aryl radical including from 6 to 10 carbon atoms, an alkyloxycarbonyl group including from 2 to 5 carbon atoms, or a cyano group, or a see diagramm : EP0050534,P46,F4 group, in which B' represents an oxygen or sulphur atom, a see diagramm : EP0050534,P46,F5 or -CH2 - group or a sulphoxide group or a sulphone group and R4 represents a hydrogen atom, a -C=-CN radical, a methyl radical, a -CONH2 radical, a -CSNH2 radical or a -C=-CH radical, R5 represents a halogen atom or a methyl radical and n represents a numeral, 0, 1 or 2, and in particular the 3-phenoxybenzyl, alpha-cyano-3-phenoxybenzyl, alpha-ethynyl-3-phenoxybenzyl, 3-benzoylbenzyl, 1-(3-phenoxyphenyl) ethyl or alpha-thioamido-3-phenoxybenzyl group, or a see diagramm : EP0050534,P47,F1 group, or a see diagramm : EP0050534,P47,F2 group, in which the substituents R6 , R7 , R8 , R9 represent a hydrogen atom, a chlorine atom, or a methyl radical and in which S/l symbolises an aromatic ring or an analogous dihydro or tetrahydro ring, or a see diagramm : EP0050534,P47,F3 group or a see diagramm : EP0050534,P47,F4 group, in which R10 represents a hydrogen atom or a CN radical, R12 represents a -CH2 -radical or an oxygen atom, R11 represents a thiazolyl or a thiadiazolyl radical, whose bond with see diagramm : EP0050534,P47,F5 can be found at any one of the available positions, R12 being linked to R11 by the carbon atom contained between the sulphur atom and a nitrogen atom, or a see diagramm : EP0050534,P48,F1 group 1. a see diagramm : EP0050534,P48,F1 group or a see diagramm : EP0050534,P48,F2 group in which R13 represents a hydrogen atom or a CN radical, or a see diagramm : EP0050534,P48,F3 group in which R13 is defined as above, and the benzoyl radical is at position 3 or 4, or a see diagramm : EP0050534,P48,F4 group in which R14 represents a hydrogen atom, a methyl, ethynyl or cyano radical and each of R15 and R16 being different, represents a hydrogen, fluorine or bromine atom, or a see diagramm : EP0050534,P48,F5 group in which R14 is defined as above, each of the R17 'S represents independently an alkyl group containing from 1 to 4 carbon atoms, an alkoxy group containing from 1 to 4 carbon atoms, an alkylthio group containing from 1 to 4 carbon atoms, an alkyl sulphonyl group containing from 1 to 4 carbon atoms, a trifluoromethyl group, a 3,4-methylene dioxy group, or a chloro, fluoro or bromo group, p represents a numeral 0, 1 or 2 and B' represents an oxygen atom or a sulphur atom. 1. Claims (for the Contracting State AT) Process for preparing, in all possible isomeric forms, or in the form of a mixture of isomers, the compounds with the formula I : see diagramm : EP0050534,P52,F3 in which R represents either a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing from 1 to 8 carbon atoms, possibly substituted by one or more functional groups, identical or different, or an aryl group containing from 6 to 14 carbon atoms, possibly substituted by one or more functional groups, identical or different, or a heterocyclic radical possibly substituted by one or more functional groups, identical or different, B represents either a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing from 1 to 18 carbon atoms, or the residue of an alcohol used in the synthesis of esters of the pyrethrinoid series and X represents a halogen atom, the ethylene double bond having the geometry Z or E, characterized in that an acid with the formula II : see diagramm : EP0050534,P52,F4 in which X and R retain the same significance as previously, this acid being in the form of mixtures of E or Z isomers or in the form of an E or Z isomer, the substituted cyclopropane ring being able to be in all its possible sterio-isomeric forms, or in the form of a mixture of stereo-isomers or a functional derivative of this acid, is made to react with an alcohol with the formula III : where B retains the same significance as previously or with a functional derivative of this alcohol, so as to obtain a corresponding compound with the formula I, which if desired, is submitted to the action of a selective cleavage agent of the CO2 R group so as to obtain a compound with the formula IV : see diagramm : EP0050534,P53,F1 in which B retains the same significance as previously, then, this acid with the formula IV or a functional derivative of this acid, is submitted to the action of an alcohol with the formula R-OH in which R retains its previous significance, so as to obtain a corresponding compound with the formula I.

专利号:US-2007275962-A1
优先权日:2003-09-10
标 题:Heterobicyclic Compounds as Pharmaceutically Active Agents
发明人：KOUL ANIL; KLEBL BERT; MULLER GERHARD; MISSIO ANDREA; SCHWAB WILFRIED; HAFENBRADL DORIS; NEUMANN LARS; SOMMER MARC-NICOLA; MULLER STEFAN; HOPPE EDMUND; FREISLEBEN ACHIM; BACKES ALEXANDER; HARTUNG CHRISTIAN; FELBER BEATRICE; ZECH BIRGIT; ENGKVIST OLA; KERI GYORGY; ORFI LASZLO; BANHEGYI PETER; GREFF ZOLTAN; HORVATH ZOLTAN; VARGA ZOLTAN; MARKO PETER; PATO JANOS; SZABADKAI ISTVAN; SZEKELYHID ZSOLT; WACZEK FRIGYES
权利人:GPC BIOTECH AG
摘要:Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.