8-氯-10,11-二氢-4-氮杂-5H-二苯并a,d-5-环庚酮的合成
Synthesis of 8-Chloro-10,11-dihydro-4-aza-5H-dibenzoa,d cyclohepten-5-one
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摘要: 以2-氰基-3-甲基吡啶为原料,通过Ritter反应、烷基化、腈化、水解、环化等五步反应成了氯雷他定的重要中间体8-氯-10,11-二氢杂-5H-二苯并a,d-5-环庚酮,总收率为25.6%,其结构经核磁共振、质谱等确证。Abstract: Chloro-10,11-dihydro-4-aza-5H-dibenzoa,dcyclohepten-5-one is an important intermediate of loratadine.It was synthesized from 2-cyano-3-methylpyridine as the starting material via Ritter reaction, alkylation, cyanidation, hydrolysis and cyclization under mild conditions. The total yield attained was 25.6%. The chemical structure was confirmed by means of 1 H-NMR,MS and m.p.data.