Method for preparing safe and effective antibechic dimimorfan phosphate
A technology of dimethylmorphine phosphate and dimethylmorphine, which is applied in the field of drug synthesis and can solve the problems of harsh reaction conditions, low product yields, and high production costs
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[0015] The present invention uses dextromorphan as a raw material, and only needs to go through three steps of esterification, methylation and salt formation to prepare the target product dimethylorphane phosphate, and the reaction yield of each step reaches more than 80%, and the operation Simple and economical. The method is as follows:
[0016] 1. Esterification, with dextrohydroxymorphan as raw material, under the condition of nitrogen protection, with CF 3 SO 2 Cl reacts to generate dextrohydroxymorphan trifluoromethanesulfonyl ester;
[0017] 2. Methylation, using toluene as a solvent, dextrohydroxymorphan trifluoromethanesulfonyl ester reacts with tetramethyltin under the catalysis of bistriphenylphosphine palladium dichloride to form dimethylorphane or dextrohydroxymorph Trifluoromethanesulfonyl ester reacts with methylmagnesium bromide under the action of iron acetylacetonate as a catalyst to generate dimerphane with THF as a solvent;
[0018] 3. Salt formation, d...
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