An Optimized Safe Process from Bench to Pilot cGMP Production of API Eptifibatide Using a Multigram-Scale Microwave-Assisted Solid-Phase Peptide Synthesizer

Autor: Paolo Rovero, Alfredo Paio, Annunziata D’Ercole, Matteo Zini, Francesca Nuti, L. Pacini, Anna Maria Papini, Arianna Ribecai, Giuseppina Sabatino

Publikováno v: Organic process research & development 25 (2021): 2754–2771. doi:10.1021/acs.oprd.1c00368
info:cnr-pdr/source/autori:D'Ercole, Annunziata; Pacini, Lorenzo; Sabatino, Giuseppina; Zini, Matteo; Nuti, Francesca; Ribecai, Arianna; Paio, Alfredo; Rovero, Paolo; Papini, Anna Maria/titolo:An Optimized Safe Process from Bench to Pilot cGMP Production of API Eptifibatide Using a Multigram-Scale Microwave-Assisted Solid-Phase Peptide Synthesizer/doi:10.1021%2Facs.oprd.1c00368/rivista:Organic process research & development/anno:2021/pagina_da:2754/pagina_a:2771/intervallo_pagine:2754–2771/volume:25

A growing industrial interest toward the peptide drug market fueled the need for the development of effective and cGMP compliant manufacturing methods for these complex molecules. Solid-phase strategies are considered methods of election for medium-l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d29c2a766b49246c4ffd343dfd85a016
https://publications.cnr.it/doc/464122

Mild and convenient one-pot synthesis of 1,3,4-oxadiazoles

Autor: Paolo Stabile, Giuseppe Guercio, Damiano Castoldi, Ornella Curcuruto, Arianna Ribecai, Alessandro Lamonica

Publikováno v: Tetrahedron Letters. 51:4801-4805

A mild, general, convenient, and efficient one-pot synthesis of 2-phenyl-5-substituted-1,3,4-oxadiazoles is described. Both (hetero)aryl and alkyl carboxylic acids were efficiently condensed with benzohydrazide in the presence of TBTU to give diacylh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::00484cc4bc23b41b86401346486aabbf
https://doi.org/10.1016/j.tetlet.2010.06.139

Overall Synthesis of GSK356278: Quick Delivery of a PDE4 Inhibitor Using a Fit-for-Purpose Approach

Autor: Paolo Stabile, Arianna Ribecai, Nicola Giubellina, Sara Rossi, Giuseppe Guercio, Lucilla Turco, Claudio Bismara, Riet Dams, Pieter Westerduin, Damiano Castoldi, Alessandro Lamonica, Anna Nicoletti, Stefano Provera

Publikováno v: Organic Process Research & Development. 14:1153-1161

The family of phosphodiesterase (PDE) enzymes hydrolyse cyclic nucleotides, cAMP and cGMP, leading to their inactivation as intracellular second messengers. Inhibition of these enzymes leads to an elevation of levels of cyclic nucleotides in the cell

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f09bdd808d853a70a14a804585b37e4f
https://doi.org/10.1021/op1001148

Mild, convenient and versatile Cu-mediated synthesis of N-aryl-2-imidazolidinones

Autor: Arianna Ribecai, Paolo Stabile, Alessandro Lamonica, Ornella Curcuruto, Giuseppe Guercio, Damiano Castoldi

Publikováno v: Tetrahedron Letters. 51:3232-3235

A mild, general, convenient and practical methodology for the selective copper-mediated mono N-arylation of unprotected 2-imidazolidinone was developed. Strong electron-donating groups and free hydroxy and amino groups on the aryl iodide substrates w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::665d8c79f72b8249befbf3f64f29ec07
https://doi.org/10.1016/j.tetlet.2010.04.064

Microwave-assisted synthesis of indole-derivatives via cycloisomerization of 2-alkynylanilines in water without added catalysts, acids, or bases

Autor: Adriano Carpita, Arianna Ribecai

Publikováno v: Tetrahedron Letters. 50:6877-6881

An unprecedented green methodology is described for the preparation of differently substituted indoles via microwave-assisted cycloisomerization of 2-alkynylaniline derivatives in water. Moderate to good yields in the cyclization can be achieved for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3fe8beccd89359b34e14473187770ba1
https://doi.org/10.1016/j.tetlet.2009.09.135