CAS: 124-87-8; Picrotoxin,1:1Mixtureofpicrotoxininandpicrotin

专利信息

专利号:US-12428656-B2
优先权日:2020-02-28
标题 :Nitrilase mutant and application thereof in the synthesis of 1-cyanocyclohexyl acetic acid
发明人：XUE YAPING; XIONG NENG; LI QIAN; ZHENG YUGUO
权利人:UNIV ZHEJIANG TECHNOLOGY
摘要:The present invention provides a nitrilase mutant and application thereof in the synthesis of 1-cyanocyclohexyl acetic acid, the nitrilase mutant is obtained by mutating one or two of the amino acids at position 180 and 205 of the amino acid sequence shown in SEQ ID No. 2. In the present invention, by semi-rational design and protein molecular modification, the specific enzyme activity of the nitrilase double mutant AcN-G180D/A205C was increased by up to 1.6 folds, and the conversion rate>99%. And the reaction time was shortened to a quarter of the original using the recombinant Escherichia coli containing the nitrilase mutant to hydrolyze 1-cyanocyclohexylacetonitrile at high temperature (50° C.). Therefore, the mutants obtained by the present invention have a good application prospect in efficiently catalyzing 1-cyanocyclohexylacetonitrile to synthesize gabapentin intermediate, 1-cyanocyclohexyl acetic acid.

专利号:US-6409988-B1
优先权日:1999-07-01
标 题:Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands
发明人：DHANOA DALJIT S; MEEGALLA SANATH; DOLLER DARIO; SOLL RICHARD M
权利人:DIMENSIONAL PHARM INC
摘要:The present invention is directed to radiolabeled compounds of Formula I:or salts thereof, whereR1 represents R8, R8O, R8SO2, R8SO or R8S in which R8 is tritiated or deuterated methyl;X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substitutedC6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond;R2 is hydrogen or amino; andR3-R7 are defined in the specification.The invention is also directed to methods of using such compounds for demonstrating specific insect GABA receptors, qualitatively screening for compounds acting on an insect GABA receptor or quantitatively assaying concentrations of a compound acting on an insect GABA receptor.

专利号:US-2022372531-A1
优先权日:2020-02-28
标题:A nitrilase mutant and application thereof in the synthesis of 1-cyanocyclohexyl acetic acid

专利号:US-5089639-A
优先权日:1988-09-01
标题:N-cycloalkylalkylamines, process for their preparation, their use as a medicament and their synthesis intermediates
发明人：AUBARD GILBERT G; CALVET ALAIN P; DEFAUX JEAN-PIERRE; GOURET CLAUDE J; GROUHEL AGNES M; JACOBELLI HENRY L; JUNIEN JEAN-LOUIS; PASCAUD XAVIER B; ROMAN FRANCOIS F; HUDSPETH JAMES P; LIN YUAN
权利人:JOUVEINAL SA
摘要:N-Cycloalkylalkylamines of formula I: ##STR1## in which: R1 is phenyl which is optionally mono-, di- or trisubstituted by halogens or lower alkyl, haloalkyl or lower alkoxy radicals, or is an aromatic heterocyclic radical having 5 to 7 chain members, in which the hetero atom is nitrogen, oxygen or sulphur, n R2 is lower alkyl, n R3 is hydrogen or lower alkyl, n m has the value of 1 or 2, n R4 is cycloalkyl --CH(CH2)n, in which a carbon atom may carry a radical Rx, which is lower alkyl or phenyl; and in which n has the values from 2 to 5, n R5 is phenyl, which can be mono-, di- or trisubstituted by halogens or by lower alkoxy radicals, and n Q represents an ethylene-1,2-diyl group --CHâ•?CH-- or a cyclopropane-1,2-diyl group ##STR2##

专利号:RU-2039748-C1
优先权日:1993-07-06
标题:Method of synthesis of 6,7-dihalogen -3,3-bis- (trifluoromethyl)-2-azabicyclo[2,2,1] heptanes

专利号:US-6518266-B1
优先权日:1999-07-22
标题:1- Aryl-3-thioalkyl pyrazoles, the synthesis thereof and the use thereof as insecticides
发明人：DHANOA DALJIT S; DOLLER DARIO; MEEGALLA SANATH; SOLL RICHARD M; WISNEWSKI NANCY; SILVER GARY; STINCHCOMB DAN T; SEWARD R LEE; AGRAFIOTIS DIMITRIS; SHA DEYOU
权利人:DIMENSIONAL PHARMACEUTICALS 3; HESKA CORP
摘要:The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I:or a salt thereof, whereR1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein;X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond;R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; andR3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.