摘要:
Novel substituted lactones of amino acids in all their possible stereoisomeric forms or mixtures thereof of the formula ##STR1## wherein A is a hydrocarbon chain of 1 to 10 chain members containing one or more heteroatoms and one or more unsaturations and the chain members being a mono- or polycyclic system or comprises a system of spiro or endo type and may contain one or more chiral atoms or the lactone copula can present a supplementary chirality due to the asymetric spatial configuration of the molecule make up and R is selected from the group consisting of ##STR2## wherein Z is the organic remainder of an amino acid of the formula ##STR3## Y is derived from a primary, secondary or tertiary alcohol of the formula Y--OH and B is the remainder of a heterocyclic amino acid of 3 to 6 carbon atoms of the formula ##STR4## and their preparation and their use for the resolution of amino acids.
摘要:
Novel esters in all possible isomeric forms and mixtures thereof of the formula ##STR1## wherein A is selected from the group consisting of ##STR2## R is selected from the group consisting of hydrogen, --CN and --C.tbd.CH, Y is selected from the group consisting of oxygen and sulfur, Z is selected from the group consisting of alkyl and alkoxy of 1 to 4 carbon atoms, alkylthio and alkylsulfonyl of 1 to 4 carbon atoms, cycloalkyl of 3 to 4 carbon atoms, 3,4-methylenedioxy, chlorine, fluorine and bromine, n is an integer of 0, 1 or 2, Z.sub.1 and Z.sub.2 may both be methyl or Z.sub.1 is hydrogen and Z.sub.2 is ##STR3## R.sub.3 is selected from the group consisting of hydrogen and halogen, R.sub.1 and R.sub.2 are individually alkyl of 1 to 8 carbon atoms or taken together with the carbon they are attached to form cycloalkyl of 3 to 6 carbon atoms or ##STR4## X is selected from the group consisting of oxygen and sulfur, T is at least one member of the group consisting of halogen, alkyl of 1 to 8 carbon atoms, alkoxy of 1 to 8 carbon atoms optionally substituted with at least one halogen and --CF.sub.3 and m is an integer from 0, 1 or 2 having insecticidal activity as well as nematocidal and acaricidal activity.
摘要:
Antiandrogenic compositions comprising an effective amount of at least one compound of the formula ##STR1## wherein X and Y are individually selected from the group consisting of hydrogen, halogen, --CF.sub.3, --NO.sub.3 and alkylthio of 1 to 4 carbon atoms and R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, phenyl, benzyl and hydroxymethyl and an inert pharmaceutical carrier and a method of inducing antiandrogenic activity in warm-blooded animals as well as novel oxadiazines of formula I with the proviso that when R is other than benzyl or hydroxymethyl at least one of X and Y is alkylthio of 1 to 4 carbon atoms.
摘要:
An insecticidal composition comprising an insecticidally effective amount of (S) .alpha.-cyano-3-phenoxy-benzyl(1R, trans) 2,2-dimethyl-3-[(.DELTA.Z) 2-fluoro-3-oxo-3-methoxy-propenyl]-cyclopropane carboxylate and an inert carrier having excellent insecticidal activity and low mammal toxicity.
摘要:
Novel esters in all possible isomeric forms of the formula ##STR1## wherein R is selected from the group consisting of (a) optionally unsaturated alkyl of 1 to 8 carbon atoms and optionally unsaturated cycloalkyl or cycloalkyl-alkyl of 3 to 8 carbon atoms optionally substituted with at least one member of the group consisting of halogen, --OH, --SH, --OR', --SR', --NO.sub.2, ##STR2## --CN, --SO.sub.3 H, --PO.sub.4 H.sub.2, ##STR3## --SO.sub.2 AlK.sub.2, --SO.sub.3 AlK.sub.3, aryl optionally substituted with at least one member of the group consisting of --OH, alkoxy of 1 to 8 carbon atoms, alkyl of 1 to 8 carbon atoms, halogen, --CF.sub.3, --OCF.sub.3, --SCF.sub.3 and ##STR4## R' is alkyl of 1 to 8 carbon atoms, R" and R"' are individually selected from the group consisting of hydrogen and alkyl of 1 to 8 carbon atoms, AlK.sub.1, AlK.sub.2 and AlK.sub.3 are individually alkyl of 1 to 18 carbon atoms, (b) aryl of 6 to 14 carbon atoms optionally substituted with at least one substitutent selected from the group consisting of --OH, alkoxy of 1 to 8 carbon atoms, alkyl of 1 to 8 carbon atoms, halogen, --OCF.sub.3, --CF.sub.3 and --SCF.sub.3 and (c) heterocycle optionally substituted with at least one member of the group consisting of --OH, alkoxy of 1 to 8 carbon atoms, alkyl of 1 to 8 carbon atoms, halogen, --CF.sub.3, --OCF.sub.3 and --SCF.sub.3, B is selected from the group consisting of optionally unsaturated alkyl of 1 to 18 carbon atoms, optionally unsaturated cycloalkyl of 3 to 18 carbon atoms and the remainder of an alcohol used in synthesis of pyrethrinoid esters, X is halogen and the ethylenic double bond may have Z or E geometry having parasitic activity, especially insecticidal acaricidal and nematocidal activity.
摘要:
Novel isomers and mixtures thereof of cyclopropane carboxylic acid derivatives with a 3-unsaturated side chain of the formula ##STR1## wherein A' is selected from the group consisting of wherein B is selected from the group consisting of --CH.sub.2 --, ##STR2## --O-- and --S--, R.sub.4 is selected from the group consisting of hydrogen, --CH.sub.3,--C.tbd.N--CONH.sub.2, --CSNH.sub.2 and --C.tbd.CH, n is an integer from 0, 1 or 2 and R.sub.5 is selected from the group consisting of halogen and --CH.sub.3 ##STR3## wherein R.sub.13 is selected from the group consisting of hydrogen and ##STR4## wherein R.sub.13 has the above definition and the benzoyl is in the 3- or 4-position, ##STR5## wherein R.sub.14 is selected from the group consisting of hydrogen, methyl, ethynyl and --CN and R.sub.15 and R.sub.16 are individually selected from the group consisting of hydrogen, bromine and fluorine and ##STR6## wherein R.sub.14 has the above definition, p is 0, 1 or 2, each R.sub.17 is selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms, alkylsulfonyl of 1 to 4 carbon atoms, --CF.sub.3, 3,4-methylenedioxy, chlorine, bromine and fluorine B' is selected from the group consisting of --O-- and --S-- and R is selected from the group consisting of alkyl of 1 to 18 carbon atoms substituted with one or more, optionally different functional groups, aryl of 6 to 14 carbon atoms optionally substituted with one or more optionally different functional groups, the double bond having Z or E geometry having insecticidal and nematocidal activity as well as plant and animal acaricidal activity and their preparation.
摘要:
Novel ethers of organic compounds containing chiral atoms of the formula ##STR1## wherein A is a hydrocarbonated chain of 1 to 10 groups, the said chain containing one or more heteroatoms, one or more unsaturations, the assembly of the groups constituting the chain may represent a mono- or polycyclic system, including a system of the spiro or endo type, the chain A can contain one or more chiral atoms or the lactone moiety can present a chirality due to the dissymetric spatial configuration of the whole of the molecule and Z is selected from the group consisting of primary, secondary or tertiary alcohol moiety containing at least an asymetric carbon atom, a phenol moiety substituted comprising at least one asymetric carbon atom and a substituted alcohol or phenol moiety with a chirality due to the dissymetric spatial configuration of the whole of the molecule, with the proviso Z is not (R) or (S) .alpha.-cyano-3-phenoxy-benzyl when A is ##STR2## which are useful for the resolution of compounds of the formulae ##STR3## wherein A and Z have the above definitions and X is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms.
摘要:
Novel esters of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of carbamoyl and R.sub.1 ' and R.sub.2 ', R.sub.1 ' and R.sub.2 ' are individually selected from the group consisting of hydrogen, halogen, alkyl of 1 to 6 carbon atoms, aryl of 6 to 10 carbon atoms, aralkyl of 7 to 13 carbon atoms, alkoxycarbonyl of 2 to 5 carbon atoms and --CN, R.sub.3 and R.sub.3 ' are individually selected from the group consisting of hydrogen, halogen, alkenyl of 2 to 3 carbon atoms and alkyl of 1 to 3 carbon atoms, Y' is selected from the group consisting of ##STR2## R.sub.4 ' and R.sub.5 ' are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, fluorine, bromine, chlorine and R.sub.4 ' and R.sub.5 ' together with the carbon atom to which they are attached form an optionally unsaturated hydrocarbon ring or heterocycle of 3 to 7 chain members and a heterocycle of the formula X is selected from the group consisting of sulfur and oxygen or R.sub.4 ' is cyano and R.sub.5 ' is phenyl or R.sub.4 ' is hydrogen and R.sub.5 ' is selected from the group consisting of cyano, ##STR3## AlK is alkyl of 1 to 4 carbon atoms, the double bond in the 1- position of the vinyl side chain of formula (A) having (E) or (Z) configuration, R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and alkoxycarbonyl of 2 to 5 carbon atoms, the substituents on the cyclopropane ring of formula (A) and (C) have the cis or trans, racemic or optically active configuration, Z.sub.1 is alkyl of 1 to 4 carbon atoms, Z.sub.2, Z.sub.3 and Z.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkylthio of 1 to 4 carbon atoms and halogen and the asymetric carbon of formula (D) may be (S) or (R) configuration or a racemic mixture thereof and the carbon atom in the 1- position of the alcohol moiety may have (R), (S) or racemic configuration having insecticidal properties and their preparations.
摘要:
Novel substituted lactones of amino acids in all their possible stereoisomeric forms or mixtures thereof of the formula ##STR1## wherein A is a hydrocarbon chain of 1 to 10 chain members containing one or more heteroatoms and one or more unsaturations and the chain members being a mono- or polycyclic system or comprises a system of spiro or endo type and may contain one or more chiral atoms or the lactone copula can present a supplementary chirality due to the asymetric spatial configuration of the molecule make up and R is selected from the group consisting of: ##STR2## wherein Z is the organic remainder of an amino acid of the formula: ##STR3## Y is derived from a primary, secondary or tertiary alcohol of the formula Y-OH and B is the remainder of a heterocycle amino acid of 3 to 6 carbon atoms of the formula: ##STR4## and their preparation and their use for the resolution of amino acids.