| 摘要 |
Novel compounds of the formula <FORM:1095236/C2/1> wherein R is C1- 5 alkyl, cyclo-alkyl, trihalo-methyl-C1- 4 alkyl or a phenyl or phenyl-C1- 5-alkyl group optionally bearing halogen or C1- 5 alkyl or alkoxy substituents on the phenyl ring; R1 is H, C1- 5 alkyl or C1- 6 alkanoyl; X is H, halogen or C1- 5 alkyl or two X radicals on adjacent atoms of the benzene ring may together form a divalent 4 carbon atom hydrocarbon radical, e.g. -CH=CH-CH=CH-, m=1-3 and n=1-5, and salts, esters and amides of these compounds are made by reacting a Mannich base of the formula <FORM:1095236/C2/2> wherein R2 and R3 are C1- 5 alkyl groups or NR2R3 forms a heterocyclic ring and HA represents an acid capable of forming salts with amines, with a base, e.g. aqueous NaHCO3, and, if required, esterifying, e.g. by reacting with an alcohol or by forming the acid halide and reacting with an alcohol, or converting to the amide by reacting the acid halide or an ester with ammonia or an amine. Preferred products comprise N - 4 - (2 - alkylacryloyl) phenyl - glycines and N - 4 - (2 - alkylacryloyl) phenyl - alanines optionally bearing halogen or alkyl substituents on the phenyl nucleus. Mannich compounds of Formula II are made by condensing the appropriate N-carboxy-alkyl - 4 - C2- 7 alkanoyl - aniline or its N-acyl derivative, with formaldehyde or paraformaldehyde and the acid addition salt of a secondary amine. N - Carboxyalkyl - 4 - C2- 7 alkanoyl anilines are made by reacting an N-alkanoyl aniline, optionally bearing substituents corresponding to X1, with an alkanoyl halide R.CH2COHal. in the presence of AlCl3 to give a 4-alkanoyl-acylanilide hydrolysing to form a 4-alkanoyl aniline, reacting with a haloalkanoyl ester Hal.CnH2n.COOAlkyl and hydrolysing the resulting N-carboxyalkyl-4-alkanoylaniline ester.
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