- Synthesis and characterization of process related impurities of (±)-Milnacipran
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Milnacipran is a cyclopropane derivative, used as an anti depressant drug. During the process development of milnacipran, four process related potential impurities were detected in high performance liquid chromatography. All these impurities were identified, synthesized and subsequently characterized by their respective spectral data (IR, LC-MS, 1HNMR, and 13C NMR) as described in this article.
- Raja Gopal,Christy Prabakar,Chandrashekar,Vijaya Bhaskard,Veera Somaiah
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- PROCESS FOR PREPARING LEVOMILNACIPRAN
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The present invention refers to a new process for preparing levomilnacipran, in particular to a process for the resolution of racemic tw-milnacipran with a derivative of optically active phenylglycine.
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Page/Page column 6
(2015/07/07)
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- PROCESS FOR THE PREPARATION OF (±M1R(S), 2SRR)L-2-(AMINOMETHYL)-N,N-DIETHYL-L-PHENYLCYCLOPROPANE CARBOXAMIDE HYDROCHLORIDE
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The present invention relates to an improved process for the preparation of (±)-[1R(S),2S(R)]-2-(aminomethyl)-N,N-diethyl-l-phenylcyclopropane carboxamide hydrochloride compound of formula- la.
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Page/Page column 23-24
(2012/04/23)
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- A NEW PROCESS FOR PREPARING OPTICALLY PURE MILNACIPRAN AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS.
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The present invention relates to an improved and commercially, viable process for the resolution of racemic cis milnacipran of formula I and its pharmaceutically acceptable salts of formula II. The present invention comprises using racemic cis milnacipran or its pharmaceutically acceptable salts as starting material, a low cost and commercially available resolving agent of formula III and industrially safe and economically low cost material such as water as a solvent. The said process results into optical isomers of racemic cis milnacipran having excellent optical purity without involving multiple crystallization steps. The present invention also comprises the concept of green chemistry as the invention works well with water as a solvent thereby minimizing the use of any other solvent. (Formular I and II should be inserted here) Wherein X is anion selected from Cl, Br, I, HSO4, Phosphate or organic acid(Formular III should be inserted here) *represent asymmetric centre Compound of formula III represent mandelic acid and its derivatives.
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Page/Page column 27
(2012/05/20)
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- PROCESS FOR PREPARING OPTICALLY PURE MILNACIPRAN AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
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The present invention relates to an improved and commercially, viable process for the resolution of racemic cis milnacipran of formula I and its pharmaceutically acceptable salts of formula II. The present invention comprises using racemic cis milnacipran or its pharmaceutically acceptable salts as starting material, a low cost and commercially available resolving agent of formula III and industrially safe and economically low cost material such as water as a solvent. The said process results into optical isomers of racemic cis milnacipran having excellent optical purity without involving multiple crystallization steps. The present invention also comprises the concept of green chemistry as the invention works well with water as a solvent thereby minimizing the use of any other solvent. (Formular I and II should be inserted here) Wherein X is anion selected from Cl, Br, I, HSO4, Phosphate or organic acid (Formular III should be inserted here) *represent asymmetric centre Compound of formula III represent mandelic acid and its derivatives.
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Page/Page column 12
(2012/12/13)
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- A PROCESS FOR PREPARING OPTICAL PURE MILNACIPRAN AND ITS PHARMACEUTICALLY ACCEPTED SALTS
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The present invention discloses a process for preparing optically pure milnacipran and their pharmaceutically acceptable salts, which adopts racemic milnacipran as starting material, tartaric acid derivatives and their compositions as resolving agents to
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Page/Page column 4-5
(2009/12/07)
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- (+/-)-(Z)-2-(aminomethyl)-1-phenylcyclopropanecarboxamide derivatives as a new prototype of NMDA receptor antagonists.
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(+/-)-(Z)-2-(Aminomethyl)-1-phenylcyclopropane-N,N-diethylcarbo xamide (milnacipran, 1), a clinically useful antidepressant, and its derivatives were prepared by an improved method and were evaluated as NMDA receptor antagonists. Of these, milnacipran (1)
- Shuto,Takada,Mochizuki,Tsujita,Hase,Ono,Shibuya,Matsuda
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p. 2964 - 2968
(2007/10/02)
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- 1-Aryl-2-(aminomethyl)cyclopropanecarboxylic Acid Derivatives. A New Series of Potential Antidepressants
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A series of 1-aryl-2-(aminomethyl)cyclopropanecarboxylic acid derivatives were synthesized and evaluated as potential antidepressants.Compounds with the Z configuration were synthesized from 1-aryl-2-oxo-3-oxabicyclohexane and those with E configuration from (E)-1-phenyl-2-(hydroxymethyl)cyclopropanecarboxylic acid.The compounds were evaluated in animal tests designed to reveal potential antidepressant activity and the existence of undesirable side effects.Several derivatives were more active than imipramine and desipramine.On the basis of its activity in pharmacological animal tests of antidepressant activity and its potential lack of side effects, 1-phenyl-1--2-(aminomethyl)cyclopropane hydrochloride, midalcipran (INN), was selected for further development.This compound is currently in phase III clinical evaluation.
- Bonnaud, Bernard,Cousse, Henri,Mouzin, Gilbert,Briley, Mike,Stenger, Antoine,et al.
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p. 318 - 325
(2007/10/02)
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