NOVEL PROCESS FOR SYNTHESIZING FINGOLIMOD HYDROCHLORIDE

摘要

Provided is a process for synthesizing Fingolimod hydrochloride comprising the following steps: (1) reacting a compound (5) with a sulfhydryl compound (I) under alkaline conditions to produce a key intermediate product (6); (2) oxidizing the product (6) to produce a sulfonyl compound (7); (3) carrying out a Knoevenagel condensation reaction of the sulfonyl compound (7) with an aldehyde group compound (8) under alkaline conditions to obtain a key intermediate (9); (4) having the intermediate (9) undergo a hydrogenation reduction and at the same time carrying out an amino deprotection to obtain 5-amino-5-[2-(4-n-octylphenyl)ethyl]-2,2-dimethyl-1,3-dioxane; and then carrying out an acetonylidene deprotection in dilute hydrochloric acid and at the same time salifying to obtain Fingolimod hydrochloride.