PEG 400/cerium ammonium nitrate combined with microwave-assisted synthesis for rapid access to beta-amino ketones. an easy-to-use protocol for discovering new hit compounds

Rossino, G.; Rui, M.; Di Giacomo, M.; Rossi, D.; Collina, S.

Risultato della ricerca: Article

2 Citazioni (Scopus)

Abstract

Compound libraries are important requirement in target-based drug discovery. In the present work, a small focused compound library based on β-aminoketone scaffold has been prepared combining microwave-assisted organic synthesis (MAOS) with polymer-assisted solution phase synthesis (PASPS) and replacing reaction workup standard purification procedures with solid phase extraction (SPE). Specifically, the effects of solvent, such as dioxane, dimethylformamide (DMF), polyethylene glycol 400 (PEG 400), temperature, irradiation time, stoichiometric ratio of reagents, and catalysts (HCl, acetic acid, cerium ammonium nitrate (CAN)) were investigated to maximize both conversion and yield. The optimized protocol generally afforded the desired products in satisfying yields and purities. The designed library is a part of our current research on sigma 1 receptor modulators, a valuable tool for the identification of novel potential hit compounds.
Lingua originaleEnglish
pagine (da-a)775-
Numero di pagine12
RivistaMolecules
Volume23
Stato di pubblicazionePublished - 2018

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Organic Chemistry
  • Physical and Theoretical Chemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Molecular Medicine
  • Chemistry (miscellaneous)

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PEG 400/cerium ammonium nitrate combined with microwave-assisted synthesis for rapid access to beta-amino ketones. an easy-to-use protocol for discovering new hit compounds. / Rossino, G.; Rui, M.; Di Giacomo, M.; Rossi, D.; Collina, S.

In: Molecules, Vol. 23, 2018, pag. 775-.

Risultato della ricerca: Article

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abstract = "Compound libraries are important requirement in target-based drug discovery. In the present work, a small focused compound library based on β-aminoketone scaffold has been prepared combining microwave-assisted organic synthesis (MAOS) with polymer-assisted solution phase synthesis (PASPS) and replacing reaction workup standard purification procedures with solid phase extraction (SPE). Specifically, the effects of solvent, such as dioxane, dimethylformamide (DMF), polyethylene glycol 400 (PEG 400), temperature, irradiation time, stoichiometric ratio of reagents, and catalysts (HCl, acetic acid, cerium ammonium nitrate (CAN)) were investigated to maximize both conversion and yield. The optimized protocol generally afforded the desired products in satisfying yields and purities. The designed library is a part of our current research on sigma 1 receptor modulators, a valuable tool for the identification of novel potential hit compounds.",
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AU - Raimondi, Maria Valeria

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AB - Compound libraries are important requirement in target-based drug discovery. In the present work, a small focused compound library based on β-aminoketone scaffold has been prepared combining microwave-assisted organic synthesis (MAOS) with polymer-assisted solution phase synthesis (PASPS) and replacing reaction workup standard purification procedures with solid phase extraction (SPE). Specifically, the effects of solvent, such as dioxane, dimethylformamide (DMF), polyethylene glycol 400 (PEG 400), temperature, irradiation time, stoichiometric ratio of reagents, and catalysts (HCl, acetic acid, cerium ammonium nitrate (CAN)) were investigated to maximize both conversion and yield. The optimized protocol generally afforded the desired products in satisfying yields and purities. The designed library is a part of our current research on sigma 1 receptor modulators, a valuable tool for the identification of novel potential hit compounds.

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