- A new enantioselective synthesis of the anti-Parkinson agent safinamide
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An alternative highly enantioselective synthesis of the anti-Parkinson agent safinamide from simple, commercially available, starting materials is described. The protocol might also be useful in the synthesis of structural variants of safinamide, such as ralfinamide or related analogues. Georg Thieme Verlag Stuttgart New York.
- Reddi, Anjaneyulu,Mujahid, Mohammad,Sasikumar, Murugesan,Muthukrishnan, Murugan
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- A Two Hour Synthesis of the Anti-Parkinson Drug Safinamide Methanesulfonate
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The critical moment of the COVID-19 outbreak requires a real-time supply of therapeutic agents. Thus, time economy in the synthesis of biologically active compounds has become increasingly decisive. In this work, we developed a two hour synthesis of the a
- Higa, Vanessa M.,Omori, Alvaro T.
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p. 1433 - 1436
(2021/07/20)
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- PROCESS FOR PREPARING SAFINAMIDE
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The present invention is related to a process for preparing safinamide and salts thereof, preferably safinamide methanesulfonate, with high yields and high enantiomeric and chemical purity without the need of using highly pure intermediates. The process o
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Paragraph 0119; 0121
(2021/02/12)
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- Process for the preparation of Safinamide Mesylate intermediate
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The present application provides methods for the synthesis of intermediates in the synthesis of Safinamide or a pharmaceutically acceptable salt thereof herein Safinamide Mesylate, that is substantially free of impurities.
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Paragraph 0037; 0053-0054
(2021/02/12)
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- Synthesis and preparation of safinamide mesylate
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The invention discloses a preparation method of safinamide mesylate, which comprises the following steps: by using commercially available m-fluorobenzyl chloride and p-hydroxybenzaldehyde as initial raw materials, carrying out three-step synthesis in an o
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Paragraph 0026
(2020/10/04)
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- Alpha-aminoamide derivative and application thereof
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The invention discloses an alpha-aminoamide derivative and application thereof. Specifically, the invention relates to a novel alpha-aminoamide derivative and a pharmaceutical composition containing the compound. The invention also relates to a method for
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Paragraph 0243; 0253; 0254; 0298; 0299
(2019/02/04)
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- A high-purity sabina amide free alkali preparation method
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The present invention provides a high-purity sabina amide free alkali preparation method: the 4 - (3 - fluorobenzyloxy) benzaldehyde, ammonia propionamide, methanol is added into reaction bottle, and the adding sodium reaction, control temperature 0 - 60
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Paragraph 0011; 0017-0023
(2019/07/08)
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- PROCESS FOR THE PREPARATION OF (S)-2-[[4-[(3-FLUOROPHENYL)METHOXY]PHENYL]METHYL]AMINO PROPANAMIDE METHANESULFONATE
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The present invention relates to an improved process for the preparation of (S)-2- [[4-[(3-fluorophenyl) methoxy] phenyl] methyl] amino propanamide methanesulfonate compound of formula-1a, represented by the following structural formula: Formula-1a The pr
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Page/Page column 10-13
(2019/09/18)
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- Preparation method of medicine-safinamide mesylate for treating Parkinson's disease
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The invention discloses a preparation method of medicine-safinamide mesylate for treating Parkinson's disease. The chemical name of the safinamide mesylate is (S)-2-[4-(3-fluorobenzyloxy)benzylamino]propionamide methanesulfonate (1), and the chemical form
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- Safinamide mesylate preparation method
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The present invention belongs to the field of pharmaceutical synthesis, and provides a new safinamide mesylate preparation method. According to the present invention, m-fluorobenzyl chloride and p-hydroxybenzaldehyde are adopted as starting raw materials,
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Paragraph 0016
(2017/05/03)
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- Method for preparing industrial safinamide mesylate
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The invention relates to a method for preparing industrial safinamide mesylate, and belongs to the technical field of organic synthesis. The method comprises the steps that a compound 3-fluorobenzylchloride and a compound p-hydroxy benzaldehyde react to g
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Paragraph 0015; 0016; 0019
(2017/06/15)
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- AN IMPROVED SYNTHESIS OF ANTI-PARKINSON AGENT
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The present invention relates to an improved process for synthesis of anti-Parkinson compound of formula (I) from commercially available (R)-benzyl glycidyl ether, wherein the compound obtained has enantiopurity greater than >98%. Formula (I) wherein R1 and R2 are each independently selected from hydrogen or halogen.
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- ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS
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The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, a
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- PROCESS FOR THE PRODUCTION OF 2-[4-(3- OR 2-FLUOROBENZYLOXY)BENZYLAMINO]PROPANAMIDES WITH HIGH PURITY DEGREE
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A process for obtaining therapeutically active 2-[4-(3- and 2-(flurobenzyloxy)benzylamino]propanamides, and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower
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Page/Page column 64-65
(2009/07/17)
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- Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase
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Safinamide, (S)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}alaninamide methanesulfonate, which is in phase III clinical trials as an anti-Parkinson drug, and a library of alkanamidic analogues were prepared through an expeditious solid-phase synthesis and evaluated for their monoamine oxidase B (MAO-B) and monoamine oxidase A (MAO-A) inhibitory activity and selectivity. (S)-3-Chlorobenzyloxyalaninamide (8) and (S)-3-chlorobenzyloxyserinamide (13) derivatives proved to be more potent MAO-B inhibitors than safinamide (IC 50 = 33 and 43 nM, respectively, vs 98 nM) but with a lower MAO-B selectivity (SI = 3455 and 1967, respectively, vs 5918). The highest MAO-B inhibitory potency (IC50 = 17 nM) and a good selectivity (SI = 2941) were displayed by (R)-21, a tetrahydroisoquinoline analogue of safinamide. Structure-affinity relationships and docking simulations pointed out strong negative steric effects of α-aminoamide side chains and para substituents of the benzyloxy groups and favorable hydrophobic interactions of meta substituents. The significantly diverse MAO-B affinities of a number of R and S α-aminoamide enantiomers, including the two rigid analogues (21) of safinamide, indicated likely enantioselective interactions at the enzymatic binding sites.
- Leonetti, Francesco,Capaldi, Carmelida,Pisani, Leonardo,Nicolotti, Orazio,Muncipinto, Giovanni,Stefanachi, Angela,Cellamare, Saverio,Caccia, Carla,Carotti, Angelo
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p. 4909 - 4916
(2008/02/13)
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- PROCESS FOR THE PRODUCTION OF 2- [4 - ( 3- AND 2-FLU0R0BENZYL0XY) BENZYLAMIN0] PROPAN AMIDES
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A process for obtaining therapeutically active 2-[4-(3- and 2- (fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower
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Page/Page column 34-35
(2008/06/13)
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- Synthesis and anticonvulsant activity of a new class of 2- [(arylalkyl)amino]alkanamide derivatives
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Although most epilepsies are adequately treated by conventional antiepileptic therapy, there remains an unfulfilled need for safer and more effective anticonvulsant agents. Starting from milacemide, a weak anticonvulsant, and trying to elucidate its mechanism of action, we discovered a structurally novel class of potent and preclinically safe anticonvulsants. Here we report the structure-activity relationship (SAR) study within this series of compounds. Different parts of the structural lead 2-[[4-(3-chlorobenzoxy)benzyl]amino]acetamide (6) were thus varied (Figure 1), and many potent anticonvulsants were found. As an outcome of this study, 57 ((S)-2-[[4-(3-fluorobenzoxy)benzyl]amino]propanamide methanesulfonate, PNU-151774E) emerged as a promising candidate for further development for its potent anticonvulsant activity and outstanding therapeutic indexes (TIs) in different animal tests.
- Pevarello, Paolo,Bonsignori, Alberto,Dostert, Philippe,Heidempergher, Franco,Pinciroli, Vittorio,Colombo, Maristella,McArthur, Robert A.,Salvati, Patricia,Post, Claes,Fariello, Ruggero G.,Varasi, Mario
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p. 579 - 590
(2007/10/03)
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