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A group of thio phosphorylation compound (by machine translation)

The present invention provides a group of thio phosphorylation compound, the compound of the formula Wherein X is or S O; R 1 is an ethyl or 2-chloro-4-bromophenyl; for R S-3-methyl-2 – (4-chlorophenyl) d acyl, 4- asian methoxy -2 – (P-chlorophenyl) – 3-cyano-5 – (trifluoromethyl) pyrrolyl, 4- asian methylthio- -2 – (P-chlorophenyl) – 3-cyano-5 – (trifluoromethyl) pyrrolyl, ethyl-(1-methylamino-2-nitro-vinyl) amino, 2-cyanoimino -1,3-thiazole alkyl in any one of; the invention discloses the structure of the compound to the agricultural insect pests and control effect, also discloses the use of these compounds as the application of the insecticide. (by machine translation)

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NEW SYNTHESES OF 2-CYANO-1-METHYL-3-<2-<<(5-METHYL-1H-IMIDAZOL-4-YL)METHYL>THIO>ETHYL>GUANIDINE (CIMETIDINE)

A new synthesis of 2-cyano-1-methyl-3-<2-<<(5-methyl-1-H-imidazol-4-yl)methyl>thio>ethyl>guanidine, 6 (cimetidine) utilizing the aziridine derivative 5 as a two-carbon one-nitrogen synthon, is reported.Attempts to prepare the key intermediate 5 via aziridine forming ring closure of 18, as well as attempted insertion of aziridine into the carbon-sulphur bond in 11 or 12 are described.Low yields of 6 were obtained both on insertion of aziridine within 12, and on alkylation of 14 with 8, followed by decomposition of the sulphonium salt 15.Formation of 5 from 2 and aziridine in the presence of Ag(I) ions is found to follow predominantly an elimination-addition mechanism, via the highly unstable carbodiimide 4, rather than direct substitution.

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PROCESS FOR PRODUCING 2-CYANOIMINO-1,3-THIAZOLIDINE

A method of obtaining a high purity 2-cyanoimino-1,3-thiazolidine, at a high yield, by cyclization reaction of dimethyl N-cyanoiminodithiocarbonate ester with 2-aminoethane thiol or the salt thereof in the presence of an alkali metal hydroxide is disclosed.

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3-Cyano-2-(N-cyanoimino)thiazolidine (3-cyano-NCT): An efficient electrophilic cyanating agent for activated methylene compounds

We found that 3-cyano-2-(N-cyanoimino)thiazolidine (3-cyano-NCT) is a novel electrophilic cyanating agent. Various activated methylene compounds were cyanated in moderate to good yields.

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3-Phosphono-2-(N-cyanoimino)thiazolidine derivatives, new phosphorylating agents for alcohols

We have developed new phosphorylating agents, 3-phosphono-2-(N-cyanoimino)-thiazolidine derivatives (3-phosphono-NCTs), which were readily synthesized by phosphorylation of NCT, and transformed primary and secondary alcohols into phosphates in good yield. The transfer of three kinds of dialkylphosphono groups [(PhO)2P(O)-, (EtO)2P(O)-, (Cl3CCH2O)2P(O)-] proceeded in excellent yields. Selective phosphorylation of various alcohols was also accomplished.

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PROCESS FOR PREPARING CYANIMINO-1,3-THIAZOLIDINES

The present invention relates to a process for preparing cyanimino-1,3-thiazolidines, which are important building blocks for the preparation of crop protection active ingredients and pharmaceuticals, by the following scheme: where A is an alkali metal and X represents an acid radical.

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An antibiotic anticancer activity method for the preparation of compounds (by machine translation)

An antibiotic anticancer active compound preparation method, comprising: cooling the ice, compound HRB-1365-0 : C4H6N2 S2, compound HRB-1365-1 : C2H7NS, and water, stirring reaction in alkaline conditions, filtration to obtain white solid, that is, for the compound HRB-1365-2 : C4H5N3S; under ice cooling, compound HRB-1365-2 : C4H5N3S, compound HRB-1365-1 : C2H7NS, triethylamine, stirring reaction in the methanol, after the completion of reaction, methanol concentrated under reduced pressure, the residue is washed with water, filtered, to obtain yellow solid is the compound HRB-1365: C6H9N3 S2; compound HRB-1365: C6H9N3 S2 of ethanol solution under stirring in the ice bath to cool down, to the drying to obtain the hydrogen chloride gas is introduced, after the saturation, continuing to stir, filtering and drying the obtained product. (by machine translation)

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2,2-Dialkylnaphthalen-1-ones as new potassium channel activators

A new series of 2,2-dialkylnaphthalen-1-one potassium channel activators has been prepared, and their in vitro relaxant activities in isolated rat portal vein and guinea pig tracheal spirals as well as their oral antihypertensive effect in spontaneously hypertensive rats have been evaluated. The group of 1,2-dihydro-4-(1,2-dihydro-2-oxo-1-pyridyl)-2,2- dimethylnaphthalen-1-ones with an electron-withdrawing substituent at the 6- position contain the most active compounds and 1,2-dihydro-4-(1,2-dihydro-2- oxo-1-pyridyl)-2,2-dimethyl-1-oxonaphthalene-6-carbonitrile, 17f (UR-8225), has been selected for further pharmacological development.

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A fluorine-containing pyridine acyl piperazine compound and use thereof (by machine translation)

The present invention provides a fluorine-containing pyridine acyl piperazine compound, structure such as shown in formula I: In the formula R is: The formula I compounds have excellent pesticidal activity, can be regarded as insecticide used for forestry insect pest of. (by machine translation)

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Reaction of 3-aralkylsulfonyl-2-(N-cyanoimino)-thiazolidines with oxygen nucleophiles

3-Aralkylsulfonyl-2-(N-cyanoimino)thiazolidines react with oxygen nucleophiles, such as sodium alkoxides and carboxylates, at the 3-sulfonyl group to give 3-alkyl- and 3-acyl-2-(N-cyanoimino)thiazolidines, respectively.

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