5751-81-5Relevant articles and documents
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Grose,Campaigne
, p. 3258 (1949)
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β-Nitroacrylates as Starting Materials of Thiophene-2-Carboxylates Under Continuous Flow Conditions
Chiurchiù, Elena,Patehebieke, Yeersen,Gabrielli, Serena,Ballini, Roberto,Palmieri, Alessandro
, p. 2042 - 2047 (2019/03/13)
We report herein a general and efficient continuous flow-based protocol for synthesizing thiophene-2-carboxylates starting from ketal-functionalized β-nitroacrylates. The protocol involves (i) a promoter-free conjugate addition of thioacetic acid to β-nitroacrylates, (ii) a base-induced elimination of nitrous acid, and (iii) a final acid-promoted domino cyclization-aromatization process to afford the title targets. Thanks to the means of the flow chemistry and the use of solid supported systems, the three steps were combined in a whole flow chemical process, by which the products were isolated in good to excellent overall yields (38–88%). (Figure presented.).
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease
Rabal, Obdulia,Sánchez-Arias, Juan A.,Cuadrado-Tejedor, Mar,de Miguel, Irene,Pérez-González, Marta,García-Barroso, Carolina,Ugarte, Ana,Estella-Hermoso de Mendoza, Ander,Sáez, Elena,Espelosin, Maria,Ursua, Susana,Haizhong, Tan,Wei, Wu,Musheng, Xu,Garcia-Osta, Ana,Oyarzabal, Julen
supporting information, p. 506 - 524 (2018/03/21)
We have identified chemical probes that act as dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors (>1 log unit difference versus class I HDACs) to decipher the contribution of HDAC isoforms to the positive impact of dua