- Preparation method of mebhydrolin napadisylate
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The invention belongs to the field of drug synthesis and provides a preparation method of mebhydrolin napadisylate. The preparation method is characterized by including the steps of firstly, subjecting methyl imine-N,N-methyl dipropionate and sodium methylate to heating under the effect of an organic solvent to achieve loop closing, and using hydrochloric acid to performing heating decarboxylationto obtain N-methyl-4-piperidone hydrochloride; subjecting phenylhydrazine and benzyl chloride to condensation under an alkaline condition to obtain benzyl phenylhydrazine; thirdly, mixing the N-methyl-4-piperidone hydrochloride solution and the benzyl phenylhydrazine, heating to generate mebhydrolin hydrochloride, adding disodium 1,5-naphthalenedisulfonate to obtain the mebhydrolin napadisylate.The preparation method is high in yield, mild in reaction conditions, convenient in intermediate purification and capable of satisfying the requirements of industrial production.
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Paragraph 0023; 0028; 0029; 0030; 0035; 0036
(2019/06/30)
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- Indole cleavage with mebhydroline by sodium periodate: Part 1: Basic substituted indoles
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The reaction behaviour of yohimbine (1), reserpine (5) and mebhydroline (7) as basic substituted indoles against periodate was examined. While 1 and 5 gave only the corresponding amine oxides 2 resp. 6 as definitive products, resulted from 7 beside the N-oxide 8 and stepwise dehydrogenation of the tetrahydro-γ-carboline to 9 and 13 also an attack at the indole system. In this ring contractions led to the spiro compounds 10 and 12 and with ring cleavage and loss of a C-1-unit the dilactam 11 was created.
- Moehrle,Nestle,Westle
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p. 445 - 452
(2007/10/03)
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