摘要:
2-Hetero-acetamido-penicillanates and cephalosporinates of the formula ##STR1## in which R is hydrogen or lower alkoxy,Z is ##STR2## R.sup.1 and R.sup.2 independently or together are various radicals, A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## n is 1 or 2, X is S,O,SO,SO.sub.2 or --CH.sub.2 --,Y is the balance of a penicillin or cephalosporin moiety, andB is a heterocyclic radical, in the form of the acid, a hydrate thereof, a salt thereof or a salt of the hydrate, exhibit marked anti-bacterial properties rendering them suited for use as antibiotics and animal feed supplements.
摘要:
Antibacterially active and animal feedstuff supplement .beta.-lactam antibiotics of the formula ##STR1## in which R is H or --UR',U is O or S,R' is optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl or cycloalkyl,Z is ##STR2## R.sup.1 and R.sup.2 individually are hydrogen or, individually or together with the carbon atom to which they are bonded, are any of various radicals,A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## B is optionally substituted phenyl or is cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO.sub.2 or --CH.sub.2 --; andY is a group of the formula ##STR4## T is hydrogen, alkyl--CO--O--, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, hydroxyl or optionally substituted --S--phenyl, or is --S--Het, in whichHet is an optionally substituted heterocyclic 5-membered or 6-membered ring; and whereinE is hydrogen, a radical forming, with the carboxyl group to which it is attached, a carboxy ester group, a cation of a salt, or a protective group,or a hydrate thereof. A process is also given for converting R directly from H to UR' employing a base, a halogenating agent and R'UH .
摘要:
2-Hetero-acetamido-penicillanates and cephalosporinates of the formula ##STR1## in which R is hydrogen or lower alkoxy,Z is ##STR2## R.sup.1 and R .sup.2 independently or together are various radicals, A is --CH.sub.2 --CH.sub.2 --,--CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## n is 1 or 2, X is S,O,SO,SO.sub.2 or --CH.sub.2 --,Y is the balance of a penicillin or cephalosporin moiety, andB is a heterocyclic radical, in the form of the acid, a hydrate thereof, a salt thereof or a salt of the hydrate, exhibit marked anti-bacterial properties rendering them suited for use as antibiotics and animal feed supplements.
摘要:
Antibacterially active and animal feedstuff supplement .beta.-lactam antibiotics of the formula ##STR1## in which R is H or --UR',U is O or S,R' is optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl or cycloalkyl, ##STR2## R.sup.1 and R.sup.2 individually are hydrogen or, individually or together with the carbon atom to which they are bonded, are any of various radicals,A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## B is optionally substituted phenyl or is cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO.sub.2 or --CH.sub.2 --; andY is a group of the formula ##STR4## T is hydrogen, alkyl-CO-O-, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, hydroxyl or optionally substituted -S-phenyl, or is -S-Het,in whichHet is an optionally substituted heterocyclic 5-membered or 6-membered ring;and whereinE is hydrogen, a radical forming, with the carboxyl group to which it is attached, a carboxy ester group, a cation of a salt, or a protective group,or a hydrate thereof. A process is also given for converting R directly from H to UR' employing a base, a halogenating agent and R'UH.
摘要:
New penicillins of the formula ##STR1## in which ##STR2## E is oxygen or sulphur, and R.sub.1 and R.sub.2 are hydrogen or various organic radicals with certain provisos,or salts thereof, are antibacterially ative and useful as antibiotics in pharmacy, as animal feed supplements for promoting growth, and as preservatives.
摘要:
A process for the preparation of the (+)-antipode of (E)-1-cyclohexyl-4,4-dimethyl-3-hydroxy-2-(1,2,4-tri-azol-1-yl)-pent -1-ene of the formula ##STR1## which comprises reacting the (E)-isomer of 1-cyclohexyl-4,4-dimethyl-2-(1,2,4-triazol-1-yl)-pent-1-en-3-one of the formula ##STR2## with lithium aluminum hydride in the presence of an inert organic diluent and in the presence of a chiral amino alcohol at a temperature between -80.degree. C. and +50.degree. C. The (+)-antipode is produced in high selectivity, using (+)-N-methyl-ephedrine.
摘要:
New solid formulations ofA) at least one agrochemical active compound,B) at least one additive from the groups mentioned in the description,C) at least one dispersant,D) at least one carrier andE) if appropriate, further active compounds and/or additives,a process for preparing the solid formulations and their use for treating plants.A new device for preparing new granules.
摘要:
A process for the preparation of a phosphoric acid propargyl ester of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is an aryl radical or a C.sub.1-4 -alkyl, C.sub.1-4 -alkenyl or C.sub.1-4 -alkynyl radical, andX, Y and Z each independently is oxygen or sulphur, comprising reacting a phosphoric acid monoester chloride or diester chloride with at least the equivalent amount of propargyl alcohol in a two-phase system in the presence of an inorganic base as an acid-trapping agent, and a catalyst comprising about 0.001 to 100 mol %, relative to the phosphoric acid ester chloride, of a tertiary amine or quaternary ammonium or phosphonium salt with at least 9 C atoms. Advantageously the catalyst is present in about 0.01 to 10 mol % relative to the phosphoric acid ester chloride and is a tertiary amine or quaternary ammonium salt, X, Y and Z are oxygen, R.sup.1 is propargyl and R.sup.2 is C.sub.1-4 -alkyl, the reaction is effected in the presence of methylene chloride, chloroform or toluene as solvent, the base is used in at least the equivalent amount and is selected from the group consisting of alkali metal hydroxides, alkaline earth metal hydroxides, alkali metal carbonates and alkaline earth metal carbonates.
摘要:
A process for the preparation of an oxirane of the formula ##STR1## in which X is 4-chlorobenzyl, 4-phenylphenoxy or 1H-(1,2,4)-triazolyl,comprising reacting dimethyl sulphate with an excess of dimethyl sulphide thereby to form trimethylsulphonium methyl-sulphate of the formula(CH.sub.3).sub.3 S.sym.CH.sub.3 SO.sub.4 .crclbar.,and without prior isolation reacting the trimethylsulphonium methyl-sulphate with a keytone of the formula ##STR2## in the presence of solid potassium hydroxide or sodium hydroxide in dimethyl sulphide at a temperature between 0.degree. C. and 50.degree. C.
摘要:
A simplified process for preparing the known insecticide 0,S-dimethylthiolphosphoric acid amide of the formula ##STR1## inexpensively, in high purity and with minimum waste water and gas which would have to be specially treated to avoid environmental pollution, comprises(a) contacting 0,0 dimethyl-thiophosphoric acid amide of the formula ##STR2## in which Me is sodium or potassium, separating the aqueous phase,(b) optionally adding an organic solvent to the aqueous phase, and reacting the mass with methyl bromide or methyl chloride thereby to form the 0,S-dimethyl-thiolphosphoric acid amide, and either(c) extracting the amide with a sparingly water-miscible solvent thereby to dissolve the amide, or(d) concentrating the reaction mixture from the methylation step (b), by distillation, until the alkali metal halide formed has separated out, and filtering off the alkali metal halide.