摘要:
PURPOSE:To obtain a carbonyl compound, having fluorine atom at the alpha-position or an alpha,beta-unsaturated carbonyl compound, having fluorine atom at the alpha-position and useful as a medicine, agricultural chemical or intermediate therefor, by reacting an enol compound with an N-fluoropyridinium salt. CONSTITUTION:An enol compound expressed by formula I (M is H, alkyl, aryl, acyl, etc.; R is H, alkyl, aryl, alkoxy, etc.; R -Ru5 are H, alkyl, alkenyl, etc.; n is 0 or 1) is reacted with a compound expressed by formula II (R -R are H, alkyl, aryl, etc., or may have a cyclic structure by various combinations), preferably in a solvent, e.g. CH2Cl2 or THF, at -80-+100 deg.C to afford the aimed compound expressed by formula III having good selectivity.
摘要:
NEW MATERIAL:A compound shown by formula I (R is H, OH, arylmercapto or arylsulfonyl; R is carboxyl, carboxamido, hydroxymethyl, formyl, 1- acylamino-1-alkoxycarbonylmethyl, etc., or OH of R and carboxyl of R may form cyclic lactone). EXAMPLE:(3S,1'S)-N-alpha-Methylbenyl-4-hydroxy-3-trifluoromethylbutanoic acid amide. USE:An intermediate for synthesizing fluorine-containing amino acid and other various compounds. R-form and S-form are obtained in 100% optical purity. PREPARATION:A compound shown by formula II (DL-form) is reacted with an optically active amine (e.g., S-(-)-alpha-phenethylamine) shown by formula III to give a compound (diastereomer mixture) shown by formula IV.
摘要:
NEW MATERIAL:A compound of formula I (X is lower alkyl; m is 0W2; R 1 , R 2 are H, lower alkyl; Y is lower alkyl, lower alkoxy, halogen; n is 0W2; where the cases where R 1 and R 2 are H and Y is lower alkyl are excluded. EXAMPLE: N-α,α-Dimethyl-4-chlorobenzyl-(1-cyclohexenyl)-acetamide. USE: Herbicide: it shows strong herbicidal effect against annual weeds in rice paddies such as barnyard grass or umbrella plant, perennial weeds such as MIZUGAYA (Cyperus serotinus ROTTB) and weeds in fields such as finger grass or smooth pigwood. PREPARATION: The reaction between a cyclohexenylacetic acid derivative of formula II or its reactive derivative and an α,α-dimethylbenzylamine derivative of formula III gives the compound of formula I . The reaction is effected in an organic solvent such as benzene in the presence of a reaction aid such as thionyl chloride. COPYRIGHT: (C)1984,JPO&Japio
摘要:
NEW MATERIAL:The compound of formulaI(R is lower alkyl; X is halogen; Y is F-substituted methyl or F-fubstituted methyloxy). EXAMPLE:N-(p-Trifluoromethyl-alpha-methylbenzyl)-alpha-bromo-t-butylac etamide. USE:An agricultural and horticultural fungicide effective remarkably to rice blast, and having rapid activity, residual activity for a long term, and low toxicity. PROCESS:The compound of formulaIcan be prepared by reacting the haloacetic acid derivative of formula II or its reactive derivative with the methylbenzylamine derivative of formula III in a solvent such as benzene, chloroform, etc. at 0 deg.C- the boiling point of the solvent, and if necessary, heating or cooling the product.