- The preparation method of the agomelatine intermediate
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The invention relates to a preparation method of an agomelatine intermediate. The method specifically comprises the following steps: by using 7-methoxyl tetrahydronaphthalene-1-one and diethyoxyl phosphoryl ethyl acetate as initial raw materials, carrying out condensation, dehydrogenation, ammonolysis and dehydration to obtain the agomelatine intermediate, namely a compound shown in a formula (IV). The preparation method provided by the invention is economical in preparation process and suitable for massively preparing the agomelatine intermediate with high yield.
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Paragraph 0028; 0030; 0031
(2018/09/26)
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- Modular Synthesis of Arylacetic Acid Esters, Thioesters, and Amides from Aryl Ethers via Rh(II)-Catalyzed Diazo Arylation
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One-pot formation of arylacetic acid esters, thioesters, and amides via Rh(II)-catalyzed arylation of a Meldrum's acid-derived diazo reagent with electron-rich arenes is described. The methodology was used to efficiently synthesize an anticancer compound.
- Best, Daniel,Jean, Micka?l,Van De Weghe, Pierre
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p. 7760 - 7770
(2016/09/12)
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- A simple and efficient procedure for synthesis of agomelatine
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A simple and efficient process for the large scale preparation of agomelatine, an antidepressant drug is described. Agomelatine was synthesized from 7-methoxy-1-tetralone in five steps. The route reported employs readily, commercially viable starting materials, reagents and potentially be utilized for the process of synthesis of agomelatine.
- Gurunadham,Raju, R. Madhusudhan,Venkateswarlu
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p. 1367 - 1370
(2016/04/08)
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- AGOMELATINE AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Agomelatine crystal, which is a drug for treating depression, and pharmaceutical compositions thereof are provided. The X-ray powder diffraction spectra of such agomelatine crystal, which is irradiated by Cu-Kα and showed by 20(degree), has characteristic diffraction peaks at 12.84, 13.84, 16.14, 18.56, 19.12, 20.86, 21.20, 23.84; its IR absorption pattern has characteristic absorption peaks at about 3234, 3060, 2940, 1638, 1511, 1436, 1249, 1215, 1184, 1032, 908, 828, 755, 588 cm-1; and its DSC endothermic transition temperature is 97.6°C. The use of the agomelatine crystal as an active ingredient in preparing a medicament for the treatment of depression is also provided.
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Page/Page column 7
(2012/07/27)
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- PROCESS FOR THE PREPARATION OF AGOMELATINE
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The present invention relates to a process for the manufacture of N-[2-(7-methoxy-1-naphthalenyl) ethyl]acetamide (Agomelatine) with improved yield and reduced level of N- acetyl-N-[2-(7-methoxy-1-naphthalenyl) ethyl]acetamide impurity.
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- SUBSTITUTED NAPHTHALENES
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Disclosed herein are substituted naphthalene-based melatonin (MT) receptor modulators and/or 5-HT receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 34-35
(2008/12/08)
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- O-arylmethyl-N-(thio)acylhydroxylamines
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The invention relates to a compound selected from those of formula (I): STR1 in which Ar, X, R 1 and R 2 are as defined in the description and a medicinal product containing the same in order to treat a disorder of the melatoninergic system.
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- Methoxybenzopyrene 4,5-Oxides Labeled with Carbon-13: Electronic Effects in the NIH Shift
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The synthesis of 9-methoxy-4,5-dihydrobenzopyrene-4-13C4,5-oxide and -5-13C4,5-oxide and of 8-methoxy-4,5-dihydrobenzopyrene-4-13C4,5-oxide is reported.The compounds were synthesized in yields of 15percent each from unlabeled precursors. 13C NMR analysis of the conversion of the 4,5-oxides to 4-phenols and 5-phenols (NIH shift) revealed a very strong electronic effect of a 9-methoxy substituent, which gave only the 4-phenol, and a significant but weaker effect of an 8-methoxy substituent, which gave both phenols with the 5-phenol predominating.
- Silverman, I. Robert,Daub, Guido H.,Jagt, David L. Vander
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p. 5550 - 5556
(2007/10/02)
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