1313876-80-0Relevant articles and documents
NOVEL PROCESS FOR SYNTHESIZING FINGOLIMOD HYDROCHLORIDE
-
Page/Page column 4, (2012/10/18)
The invention discloses a new synthetic route of Fingolimod hydrochloride, which includes the following steps: step1, reacting compound (5) with sulfhydryl compounds 1 under alkaline conditions, and obtaining key intermediate compound (6), step2, obtaining sulfone compound 7 through oxidation reaction of compound 6, step3, obtaining key intermediate compound (9) through Knoevenagel condensation reaction of the sulfone compound (7) and raw materials (aldehyde compound 8) under alkaline conditions, step4, obtaining 5- amino - 5 - [2 - (4 - N-octyl phenyl) ethyl ] - 2,2- two methyl - 1,3- two oxygen six ring through hydrogenation reduction reaction and deaminate protection of compound (9); then removing acetonide protection in the dilute hydrochloric acid solution, obtaining hydrochloride at the same time, hence getting the target compound (1) of Fingolimod hydrochloride. The advantage of the route of synthetic are as follows: the raw materials are cheap and easily obtained, and are easily to treat after reaction. It is not only to the safety of the experiment and high yield but also to reduce the pollution of the environment.