- Preparation method of agomelatine intermediate
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The invention relates to a preparation method of an agomelatine intermediate. Specifically, the invention provides a preparation method of an agomelatine important intermediate 2-(7-methoxy-1-naphthyl)acetonitrile II, 7-methoxy-1-tetralone is used as an initial raw material, condensation and oxidation reactions are carried out to obtain the intermediate 2-(7-methoxy-1-naphthyl)acetonitrile, and the preparation method has the advantages of good yield, high product purity, simple reaction and easy operation, and is suitable for industrial production .
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Paragraph 0035-0037
(2021/03/31)
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- Method and intermediate for synthesizing 7 - methoxy -1 - naphthalene acetonitrile
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The invention relates to the field of organic synthesis, and discloses a preparation method of 7 - methoxy -1 - naphthalene acetonitrile and an intermediate. The method comprises the following steps: (1) reacting 7 - methoxytetrahydro -1 -naphthyl ketone with cyanoacetic acid, (7 - methoxy -3, 4 -dihydro -1 - naphthyl) acetonitrile. (2) (7 - Methoxy -3, 4 - dihydro -1 - naphthyl) acetonitrile was subjected to a halogenation reaction to produce (7 - methoxy -3, 4 - dihydro -4 - halo -1 - naphthyl) acetonitrile. (3) (7 - Methoxy -3, 4 - dihydro -4 - halo -1 - naphthyl) acetonitrile dehalogenated hydrogen to give 7 - methoxy -1 - naphthalene acetonitrile. The method has the advantages of mild reaction conditions, less steps, simple operation and simple and easily available raw materials. There is no need to use harsh conditions, high cost catalysts or high risk chemicals. , As a new method for synthesizing 7 - methoxy -1 - naphthalene acetonitrile, the scheme provided by the invention has a good application prospect.
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Paragraph 0038-0040; 0053-0054
(2021/10/27)
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- Preparation method of 7-methoxy-1-naphthylacetonitrile
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The invention discloses a preparation method of 7-methoxy-1-naphthylacetonitrile, which is characterized by comprising the following steps of adding 7-methoxy-3, 4-dihydro-1-naphthylacetonitrile intoa first solvent, dissolving, adding allyl methacrylate, uniformly stirring, adding a catalyst ruthenium/carbon, and carrying out dehydrogenation aromatization reaction, and after the reaction is finished, filtering out the catalyst, desolventizing the filtrate under reduced pressure, adding a second solvent, heating to dissolve, cooling, crystallizing, carrying out suction filtration, and drying to obtain the white crystal 7-methoxy-1-naphthylacetonitrile. The preparation method of 7-methoxy-1-naphthylacetonitrile provided by the invention is simple to operate, less in pollution, low in cost,high in yield, less in side reaction and high in product purity, and the catalyst can be repeatedly used.
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Paragraph 0022-0023
(2020/07/24)
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- PROCESS FOR THE PREPARATION OF AGOMELATINE IN CRYSTALLINE FORM
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The present invention pertains to a process for the preparation of polymorph form X of agomelatine, which comprises providing agomelatine, and crystallizing agomelatine in the presence of at least one of an acid and a salt thereof, and to a polymorph form of agomelatine.
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- Naphthalene derivatives and their application on the medicament
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The invention provides a number of naphthalene derivatives or stereoisomers, tautomers, nitrogen oxides, metabolites, pharmaceutically acceptable salts or prodrugs thereof which are used for excitement of melatonin receptors. The invention also discloses pharmaceutical compositions containing such compounds and application thereof in treatment of central nervous system dysfunction of mammals, especially human.
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Paragraph 0229; 0230; 0231; 0232
(2016/10/09)
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- AN IMPROVED PROCESS FOR PREPARATION OF AGOMELATINE
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The present invention provides an improved process for preparing agomelatine of formula (I). The process comprises reacting 7-methoxy tetralone with cyanoacetic acid in an organic solvent to obtain (7-methoxy-3,4-dihydro- 1 -naphthalenyl)acetonitrile of Formula (B); treating compound of Formula (B) with a catalyst to obtain (7-methoxy- 1 - naphthyl)acetonitrile of Formula (C); reducing compound of formula (C) with hydrogen in presence of Raney nickel in ammoniacal methanol medium and subsequently converting to a salt using hydrochloric acid to obtain 2-(7-methoxy- 1 -naphthyI)ethanamine hydrochloride of formula (D); iv) reacting compound of formula (D) with acetic anhydride or acetic chloride in an organic solvent in presence of a base and a catalyst to obtain agomelatine of Formula (I); and optionally purifying agomelatine of Formula (I). The present invention also provides a process for preparing polymorphic Form-I of agomelatine of formula (I) comprising treating agomelatine of formula (I) in a suitable organic solvent; and isolating polymorphic Form-I of agomelatine of formula (I).
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Page/Page column 14
(2014/05/24)
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- PROCESSES FOR THE PREPARATION OF N-[2-(7-METHOXY-1-NAPHTHYL)ETHYL]ACETAMIDE
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The present invention relates to processes for the synthesis of N-[2-(7-methoxy-l - naphthethyl] acetamide, amorphous form of N-[2-(7-methoxy-l -naphthethyl] acetamide and pharmaceutical compositions thereof.
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Page/Page column 34-35
(2012/07/27)
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- Process for the synthesis of agomelatine
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Process for the industrial synthesis of the compound of formula (I)
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Page/Page column 2
(2010/03/02)
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- Process for the synthesis of (7-methoxy-1-naphthyl)acetonitrile and its application in the synthesis of agomelatine
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A process for the industrial synthesis of the compound of formula (I) Application in the synthesis of agomelatine.
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Page/Page column 5-6
(2008/06/13)
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- Process for the synthesis of (7-methoxy-3, 4-dihydro-1-naphthalenyl) acetonitrile and its application in the synthesis of agomelatine
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A process for the industrial synthesis of the compound of formula (I) Application in the synthesis of agomelatine.
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Page/Page column 3
(2008/06/13)
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- Process for the synthesis and crystalline form of agomelatine
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A process for the industrial synthesis and a new crystalline form of the compound of formula (I): Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.
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Page/Page column 6
(2008/06/13)
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