| 摘要 |
Process for the production of 4-substituted acetoacetic acid derivatives. An acetoacetic acid derivative having the formula: <IMAGE> wherein R is alkoxy having 1 to 6 C atoms, phenoxy, -NR'2, wherein R' is alkyl having 1 to 6 C atoms or aryl, or NR'2, which is azetidine, pyrrolidine or piperidine, is treated with a secondary amine at an elevated temperature and in the presence of an organic solvent. The water formed is separated. The intermediate is converted into the corresponding 3-enamine carboxylic acid derivative. The derivative is converted by treatment with sodium amide in liquid ammonia into the corresponding sodium salt. The sodium salt is converted by treatment with a halogen compound having the formula R1CH2X or R1R2CHX, wherein R1 and R2 each are alkyl, alkenyl, alkinyl or aryl and X is chlorine, bromine or iodide, into the corresponding 4-substituted enamino derivative. The derivative is hydrolyzed into the 4-substituted acetoacetic acid derivative.
|
