| abstract |
The invention discloses a preparation method of alvimopan (formula I). The method uses diethyl benzylmalonate as a starting material, and undergoes reduction with a hydride reducing agent to obtain compound VIII. VIII is combined with Vinyl acetate is reacted to obtain compound VII, VII is subjected to Jones oxidation to obtain compound VI, VI undergoes deacetylation reaction to obtain compound V, V undergoes amidation reaction to obtain compound IV, IV undergoes sulfonylation reaction to obtain compound III, III and (3R, 4R)-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine undergoes a substitution reaction to obtain compound II, and finally II undergoes ester hydrolysis to obtain alvimopan. |