Výsledky vyhledávání - "Gilles Laval"

Application of the Quality by Design Principles for the Development of the Crystallization Process for a Piperazinyl-Quinoline and Definition of the Control Strategy for Form 1

Autor: Sara Rossi, Davide Tramarin, William Maton, Brigida Allieri, Francesca Campi, Pieter Westerduin, Gilles Laval, Jason W. B. Cooke, Zadeo Cimarosti, Paolo Stabile, Nicola Giubellina

Publikováno v: Organic Process Research & Development. 16:1598-1606

The studies carried out to develop a robust crystallization method for the substituted piperazinyl-quinoline (1) a compound potentially active in the treatment of depression, are described in this contribution. These studies include the control of a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7047d1fcd161eb000d8b634507416017
https://doi.org/10.1021/op300126e

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Route Selection and Process Development for a 5-Piperazinylquinaldine Derivative for the Treatment of Depression and Anxiety

Autor: Sara Rossi, Paolo Stabile, Jason W. B. Cooke, Gilles Laval, Paola Russo, Roberta Pachera, Ramona Moretti, Pieter Westerduin, Zadeo Cimarosti, Nicola Giubellina, Francesco Tinazzi, William Maton

Publikováno v: Organic Process Research & Development. 15:1287-1296

1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone, 1, was identified as a potential drug for the treatment of depression and anxiety. Herein is described the work carried out to select the manufacturing route and the pr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f192f5af1e4d746b5fb7e9edfa63ad2c
https://doi.org/10.1021/op200140v

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Development of an Efficient Large-Scale Synthesis for a 4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide Derivative for Depression and Anxiety

Autor: Pieter Westerduin, Alcide Perboni, Zadeo Cimarosti, Gilles Laval, Paolo Stabile, Jason W. B. Cooke, Nicola Giubellina

Publikováno v: Organic Process Research & Development. 14:859-867

The development and scale-up of an optimized synthesis for a novel drug candidate for depression and anxiety is presented. The updated synthesis represents a convergent and efficient four-stage app...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a849e4d9e4ea3d5c744984d16434a0ec
https://doi.org/10.1021/op100103v

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Benzylic Brominations with N-Bromosuccinimide in (Trifluoromethyl)benzene

Autor: Claire L. Robinson, Bernard T. Golding, Shang-Min Tu, Dong Jiang, Diana Suarez, Richard Scott, Gilles Laval

Publikováno v: Synthesis. 2009:1807-1810

A variety of benzylic brominations were performed by using N-bromosuccinimide in (trifluoromethyl)benzene with photochemical activation in the presence of 2,2'-azobisisobutyronitrile, 1,1'-azobis(cyclohexanecarbonitrile), or benzoyl peroxide as the r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::aa888e817c11ab214bb736f18f1cd41b
https://doi.org/10.1055/s-0029-1216793

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Fluorination and chlorination of nitroalkyl groups

Autor: Reza Ranjbar-Karimi, Bernard T. Golding, Majid M. Sadeghi, Hossein Loghmani-Khouzani, Philip Butler, Gilles Laval

Publikováno v: Tetrahedron. 63:11160-11166

Heterocycles substituted with a nitromethyl (CH2NO2) or phenyl-nitromethyl (CHPhNO2) group were prepared by reaction of a methyl- or phenylmethyl-substituted heterocycle, respectively, with lithium di-isopropylamide followed by quenching the intermed

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::95560d524489c1b10aa578d22c8729a5
https://doi.org/10.1016/j.tet.2007.08.020

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Lipase-mediated kinetic resolution of allylic(hydroxymethyl)methylenecyclopentane building blocks

Autor: Honoré Monti, Gilles Laval, Gérard Audran, Alessandra Tolomelli, Guiliana Cardillo, Jean-Marie Galano

Publikováno v: Tetrahedron: Asymmetry. 11:1289-1294

Enzymatic-mediated kinetic acylation of allylic(hydroxymethyl)methylenecyclopentane building blocks (±)- 1a , b is reported using various commercially available lipases. Lipase Amano AK ( Pseudomonas sp.) proved to be the best lipase in the case of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2684dbc6e128027837fceaf25fa2e097
https://doi.org/10.1016/s0957-4166(00)00082-3

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Enantiospecific total synthesis of both enantiomers of laurene by a chemical diastereoselection/lipase-catalyzed kinetic resolution sequence

Autor: Gilles Laval, Sylvie Sanchez, Honoré Monti, Gérard Audran

Publikováno v: Tetrahedron: Asymmetry. 10:1927-1933

A short and efficient enantiospecific total synthesis of natural (+)-laurene and its enantiomer is described. The methodology was developed by employing a stereoselective H-ene reaction of an isocyclic allyltrimethylsilane with paraformaldehyde, foll

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cb3c921e485dc35709a771b7426767b0
https://doi.org/10.1016/s0957-4166(99)00195-0

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