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传统的环丙胺合成工艺有:①以γ-丁内酯为原料,经高压氯化、酯化、环合、胺解、Hoffmann重排合成环丙胺,该路线需在高压釜中进行,设备复杂,条件苛刻。②以1-氯-3-溴丙烷为原料与氰化钠反应生成4-氯丁腈,经环合,水解,Hoffmann降解合成环丙胺,该路线所需原料氰化钠属无机剧毒品,而且原料成本较高。③以环丙腈为原料,经水解,酰氯化,胺解,Hofmann降解合成环丙胺,该路线反应原料成本高,设备以及控制要求严格,没有应用价值。我们利用γ-丁内酯为原料,经缩合、开环、胺化、Beckmann重排和水解合成环丙胺,取得了较为满意的效果,该法具有操作简单,原料成本低,收率高,无需特殊的反应条件和设备等优点,值得工业化推广。
Traditional cyclopropanamine synthesis process: ① γ-butyrolactone as raw material, high pressure chlorination, esterification, cyclization, amine hydrolysis, Hoffmann rearrangement synthesis of cyclopropylamine, the route needs to be carried out in an autoclave, the device is complex , Harsh conditions. ② 1-chloro-3-bromopropane as raw material and sodium cyanide reaction of 4-chlorobutyronitrile, cyclization, hydrolysis, Hoffmann degradation of cyclopropylamine synthesis, the route of raw materials required sodium cyanide is an organic toxic drugs, And high cost of raw materials. ③ cyclopropanenitriles as raw materials, hydrolysis, acyl chloride, amine solution, Hofmann degradation of cyclopropylamine synthesis, the route of the reaction cost of raw materials, equipment and control requirements, there is no value. We use γ-butyrolactone as raw material, through the condensation, ring-opening, amination, Beckmann rearrangement and hydrolysis of cyclopropylamine, and achieved a more satisfactory results, the method has the advantages of simple operation, low cost of raw materials, high yield, without Special reaction conditions and equipment, etc., it is worth industrialization.