130198-05-9Relevant articles and documents
Preparation method of venlafaxine hydrochloride intermediate
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Paragraph 0032-0067, (2021/01/11)
The invention belongs to the technical field of organic synthesis, and relates to a preparation method of a venlafaxine hydrochloride intermediate, which comprises the following steps: heating, quenching, extracting, concentrating and salifying. A venlafaxine impurity C synthesized by the method is high in yield, good in purity, safe in reaction, simple to operate, free of special requirements onequipment and suitable for industrial production.
Selective Hydrogenation of Nitriles to Primary Amines Catalyzed by a Polysilane/SiO2-Supported Palladium Catalyst under Continuous-Flow Conditions
Saito, Yuki,Ishitani, Haruro,Ueno, Masaharu,Kobayashi, Shū
, p. 211 - 215 (2017/04/21)
Hydrogenation of nitriles to primary amines with heterogeneous catalysts under liquid-phase continuous-flow conditions is described. Newly developed polysilane/SiO2-supported Pd was found to be an effective catalyst and various nitriles were converted into primary amine salts in almost quantitative yields under mild reaction conditions. Interestingly, a complex mixture was obtained under batch conditions. Lifetime experiments showed that this catalyst remained active for more than 300 h (TON≥10 000) without loss of selectivity and no metal leaching from the catalyst occurred. By using this continuous-flow hydrogenation, synthesis of venlafaxine, an antidepressant drug, has been accomplished.
DERIVATIVES OF (-)-VENLAFAXINE AND METHODS OF PREPARING AND USING THE SAME
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, (2015/11/23)
Methods of preparing, and compositions comprising, derivatives of (?)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.
PROCESS FOR THE PREPARATION OF HIGHLY PURE 1-[2-DIMETHYLAMINO-(4-METHOXYPHENYL) ETHYL]CYCLOHEXANOL HYDROCHLORIDE
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Page/Page column 20, (2010/11/27)
The invention encompasses processes for the preparation of highly pure venlafaxine hydrochloride, l-[2-dimethylamino-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride as well as intermediates thereof.
PROCESS FOR PREPARATION OF 0-DESMETHYLVENLAFAXINE AND ITS ANALOGUES
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Page/Page column 12, (2008/06/13)
The present invention belongs to the field of organic chemistry and refers to a process for the preparation of O-desmethylvenlafaxine (l-[2-Dimethylamino)-l-(4-hydroxyphenyl)ethyl]cyclo- hexanol), its analogues and pharmaceutical acceptable salts thereof. The invention also relates to a catalytic hydrogenation of cyano-group of the substituted acetonitrile.
AN IMPROVED PROCESS FOR THE PREPARATION OF PURE VENLAFAXINE
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Page/Page column 9, (2008/06/13)
The present invention relates to pure Venlafaxine or salt thereof and a process for preparing highly pure Venlafaxine of structural Formula (I), Formula (I) from N, N-didesmethyl venlafaxine or salt thereof of formula (III).
A PROCESS FOR THE PREPARATION OF VENLAFAXINE HYDROCHLORIDE
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Page/Page column 11, (2008/06/13)
A process for preparing venlafaxine hydrochloride and also a process for preparing l-[2-amino- l-(4-methoxy phenyl)ethyl]cyclohexanol hydrochloride, an intermediate of venlafaxine hydrochloride are disclosed. p-Methoxy phenyl acetonitrile is condensed with cyclohexanone in the presence of a base selected from alkali metal alkoxides and solvent selected from C4 alcohol at - 10 to - 5° C to obtain l-[cyano-l-(p-methoxy phenyl)m ethyl] cyclohexanol which is directly converted it into the l-[2-amino-l-(4-methoxy phenyl)ethyl] cyclohexanol without being isolated. The molar ratio of base to p-methoxy phenyl acetonitrile or cyclohexanone used is 0.1 to 0.4:1. The l-[2-amino-l-(4-methoxy phenyl)ethyl] cyclohexanol is converted its hydrochloride salt and subsequently formylated to venlafaxine base. The venlafaxine base is further converted into its salt namely venlafaxine hydrochloride. Both venlafaxine hydrochloride and l-[2-amino-l-(4-methoxy ρhenyl)ethyl] cyclohexanol hydrochloride are obtained in high yield with high purity.
Process for the preparation of phenethylamine derivatives
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Page/Page column 5-6, (2008/06/13)
The present invention relates to a process of preparing venlafaxine and derivatives thereof comprising reducing the corresponding β-hydroxynitriles using a reducing borohydride agent selected from tetraalkylammonium borohydride and aralkyltrialkylammonium borohydride. According to the present process, said β-hydroxynitrile can be prepared by condensating a phenylacetonitrile and cyclohexanone using a phase transfer catalyst and a base at a temperature of between 10-25 °C. Advantageously, in the present method, the use of hazardous catalysts and reducing agents is avoided and unexpectedly low amounts of reducing borohydride agent can be used.
Process for the preparation of phenethylamine derivatives
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, (2008/06/13)
Disclosed is a process for the preparation of a compound of formula wherein R1 is hydrogen, hydroxyl, or unsubstituted or substituted alkyl or alkoxy, R2 is hydrogen or a substituent which can be converted to hydrogen, and n is 0, 1 or 2, comprising hydrogenating a compound of formula wherein R1, R2 and n are as defined above, in the presence of a nickel or cobalt catalyst.
