Study On Synthetic Method Of A Kind Of Terbinafine Hydrochloride

Terbinafine hydrochloride is especially at present only both may the external use and be possible to take orally compared to the naphthalene fragrance kills the fungus medicine, it has the function to the most pathogenesis fungus, in which sensitivity for the skin ringworm fungus ; Its function characteristic is: 1. medicines have lipophilic ; 2. medicine bactericidal power;3. does not affect in cytochrome oxidase CYP450, high selective action in real membrane squalene epoxidation enzyme;4. unique chemical constitutions have strongly kiss the cutin, can with the trouble department full union, and stores up in the skin in-depth。In the secure aspect, especially has following merit compared to the terbinafine hydrochloride: 1. liver toxicity are low ; 2. does not affect the internal secretion;3. does not affect other medicine metabolism; 4. side effects are slight。The skin fungus infection disease incidence rate is high, the course of an illness is long, although at present treats the medicine many, but the curative effect high, the recurrence rate low, poisonous side reaction small are really few。30 years ago promote the griseofulvin stops using because of the curative effect difference。Then alkone Kang Zuo time long treatment course treatment the poisonous side reaction is serious.Although new triazole as for example Iraq Qu Kang Zuo, fluorine Kang Zuo the curative effect is high, the side reaction is low, but its price raises generally applies with difficulty, but is especially profuse the terbinafine hydrochloride the antibacterial spectrum to be broader than, the resist bacteria affects strongly, the external use or the short treatment course oral administration may cure the major part dermatomycosis, also the recurrence rate low, the side effect few, the security is high, treats the first choice medicine which the onychomycosis and skin ringworm get sick。This article goal was to had the literature especially to conduct the research compared to the terbinafine hydrochloride process of synthesis, determined embarked from raw material N- the methyl - N- naphthalene methylamine, made the solvent by the methyl alcohol, instead earned the intermediate with the epichlorohydrine I, the intermediate I produced the intermediateⅡunder the alkalinity condition。The intermediateⅡresponded in BuLi and under the BF3-Et2O existence with uncle butyl-acetylene, obtains the intermediateⅢ; Then dehydrates, the salifying, the heavy crystal may result in the goal compound terbinafine hydrochlorid, this route synthesizes not only the terbinafine hydrochlorid the production rate is especially higher, the cost is low, moreover synthesizes the chemical reagent relative toxicity which uses to be small。...