环丙沙星关键中间体的合成

Synthesis of the key intermediate for ciprofloxacin

通过β-烯胺酮与环丙胺的串联加成消除SNAr反应的研究,建立了一种环丙沙星关键中间体7-氯-1-环丙基-6-氟-1,4-二氢-4-氧代喹啉-3-羧酸甲酯的高效合成新方法,该方法具有步骤少、产率高、后处理操作简便,适合工业化生产等优点。另外,该方法也为喹诺酮类抗菌药物的合成提供一种新思路。

A improved method has been developed for the synthesis of methyl 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate from the cyclization of β-enaminone with cyclopropanamine by a tandem addition-elimination-SNAr reaction. Simple workup procedure,good yields,short steps and suitable for scale-up are the salient features of this method. In addition,the present method offers a new synthetic access to fluoroquinolone antibiotics.