- Preparation method of meptazinol impurity D hydrochloride
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The invention provides a preparation method of meptazinol impurity D hydrochloride, successively comprising the following reaction steps: Step 1, using meptazinol hydrochloride as a raw material and washing with a first alkali solvent to obtain a free compound as shown in the formula I; Step 2, dissolving the compound as shown in the formula I in a first solvent, adding a second alkali solvent, adding Tf2O dropwise, and stirring for a period of time to obtain a compound as shown in the formula II; Step 3, carrying out a coupled reaction on the compound as shown in the formula I and the compound as shown in the formula II so as to obtain a compound as shown in the formula III; and Step 4, carrying out a reaction between the compound as shown in the formula III and a hydrochloric acid solution of methanol to obtain a compound meptazinol impurity D hydrochloride as shown in the formula V. The invention provides convenience for rapid preparation. Operation is simple; raw materials are cheap and easily available; post-treatment is simple; product purity is high; and yield is high.
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Paragraph 0048; 0049
(2019/05/08)
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- PROCESS FOR THE SYNTHESIS OF PRODRUGS OF OPIOIDS
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The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
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Page/Page column 17
(2012/07/13)
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- PRODRUGS OF OPIOIDS AND USES THEREOF
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The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are provided. The invention also provides for decreasing the adverse GI side effects of opioid analgesics.
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Page/Page column 46-47
(2011/08/08)
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- Use of weak opioids and mixed opioid agonists/antagonists for treatment of urinary incontinence
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A pharmaceutical composition for the treatment of an increased urge to urinate or urinary incontinence, comprising an effective amount of at least a compound selected from the group consisting of codeine, dihydrocodeine, dextropropoxyphene, meptazinol and tilidine. Also disclosed are methods of treatment using the pharmaceutical compositions and preferred dosages for the treatment methods.
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- Combination of selected opioids with muscarine antagonists for treating urinary incontinence
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Active compound combinations of compounds of group A, particularly opioids, and compounds of group B, particularly anti-muscarine agents and other substances suitable for treatment of an increased urge to urinate or urinary incontinence. Related pharmaceutical formulations and methods of treatment of an increased urge to urinate or urinary incontinence are also provided.
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- Hexahydroazepine, piperidine and pyrrolidine derivatives
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The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine of formula I STR1 where n is 2,3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl and R1 is lower alkyl. The compounds may be aromatized and the aromatized compounds converted to 3,3-disubstituted-hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
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- Hexahydroazepine, piperidine and pyrrolidine derivatives
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The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine derivatives of formula (I) and their aromatized derivatives of formula (II) STR1 where n is 2, 3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl, R2 is hydrogen, lower alkyl or aryl(lower)alkyl and R3 is hydrogen, lower alkyl, aryl(lower)alkyl, lower alkenyl or lower alkynyl. The compounds are useful as intermediates for preparing 3,3-disubstituted -hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
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