- Synthetic method of demethylated doxepin hydrochloride
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The invention discloses a synthetic method of demethylated doxepin hydrochloride, which comprises the following step of by using doxepin hydrochloride as an initial raw material, acylating, reducing,salifying and purifying to obtain the final product. The method overcomes the defects of harsh reaction conditions, tedious process steps, long reaction time and the like of the existing demethylateddoxepin hydrochloride synthesis process, the reaction time does not exceed 6 hours, and the whole preparation period does not exceed 10 hours, so that the preparation efficiency is greatly improved, and the preparation cost is reduced; the method has the advantages of highest product purity, highest yield and the like.
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Paragraph 0012; 0031; 0033; 0035; 0037; 0039; 0041; 0043;
(2021/01/25)
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- N-DESMETHYL-DOXEPIN AND METHODS OF USING THE SAME TO TREAT SLEEP DISORDERS
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The invention relates to desmethyldoxepin, isomers of desmethyldoxepin, and pharmaceutically acceptable salts and prodrugs of desmethyldoxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.
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Page/Page column 18
(2010/11/29)
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- Study on zwitter-ionization of drugs. II. Synthesis and pharmacological activity of some N-[3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)propyl]-N- methylamino- and N-[3-(6H-dibenz[b,e]oxepin-11-ylidene)propyl]-N-methylamino- alkanoic acid derivatives and related compounds
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A series of N-[3-(5H-dibenzo[a,d]cyclohepten-5-ylidene)propyl]-N- methylamino- (6a) and N-[3-(6H-dibenz-[b,e]oxepin-11-ylidene)propyl]-N- methylamino-alkanoic acid derivatives (6b) and related compounds (6c-f) were synthesized and examined for pharmacological activities in vitro, i.e., inhibitory effect on monoamine [noradrenaline (NA) and 5-hydroxytryptamine (5-HT)] uptake, inhibitory effect on 5-HT-, histamine-, acetylcholine- and NA-induced contraction, and binding affinity for α2-adrenoceptor and dopamine D2-receptor. In vitro tests indicated that zwitter-ionization was capable of maintaining H1-antihistaminic activity while greatly reducing other pharmacological activities. Further, 6a-f showed much stronger inhibitory effects on compound 48/80-induced lethality in rats than did the corresponding N,N-dimethylamines (2a-f). 3-[N-[3-(6H-Dibenz[b,e]oxepin-11- ylidene)propyl]-N-methylamino]-propionic acid (6b-2), selected as a candidate antiallergic agent of a new type, equally potent in rats and guinea-pigs, exhibited strong inhibitory effects on 48 h homologous passive cutaneous anaphylaxis (PCA) in rats (ED50=0.019 mg/kg, p.o.) and on histamine- induced bronchoconstriction in anesthetized guinea-pigs (ED50=0.0067 mg/kg, p.o.).
- Muramatsu,Sawanishi,Iwasaki,Kakiuchi,Ohashi,Kato,Ito
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p. 1987 - 1993
(2007/10/02)
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