6836-21-1Relevant articles and documents
The preparation method of the agomelatine intermediate
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Paragraph 0028; 0030; 0031, (2018/09/26)
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.
Modular Synthesis of Arylacetic Acid Esters, Thioesters, and Amides from Aryl Ethers via Rh(II)-Catalyzed Diazo Arylation
Best, Daniel,Jean, Micka?l,Van De Weghe, Pierre
, p. 7760 - 7770 (2016/09/12)
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.
A simple and efficient procedure for synthesis of agomelatine
Gurunadham,Raju, R. Madhusudhan,Venkateswarlu
, p. 1367 - 1370 (2016/04/08)
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.
PROCESS FOR THE PREPARATION OF AGOMELATINE
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, (2012/06/15)
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.
AGOMELATINE AND PHARMACEUTICAL COMPOSITIONS THEREOF
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, (2012/07/27)
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.
SUBSTITUTED NAPHTHALENES
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Page/Page column 34-35, (2008/12/08)
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.
O-arylmethyl-N-(thio)acylhydroxylamines
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, (2008/06/13)
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.
Methoxybenzopyrene 4,5-Oxides Labeled with Carbon-13: Electronic Effects in the NIH Shift
Silverman, I. Robert,Daub, Guido H.,Jagt, David L. Vander
, p. 5550 - 5556 (2007/10/02)
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.
