An optimised cost-effective synthesis of the new antitussive drug, DF1012, is herewith reported. The new synthetic route to the key intermediate DF1005 is based on the unusual deprotection step of the 1-tert-butyl-3-cyano-7-azaindole intermediate, which can also be regarded as a convenient way for the industrial production of the expensive 7-azaindole 1. The second key intermediate, endo-tropanamine 6, was obtained in high yield by a novel one-pot stereoselective process using a Pd-catalysed reductive amination procedure.
Allegretti, M., Anacardio, R., Cesta, M.C., Curti, R., Mantovanini, M., Nano, G., et al. (2003). A practical synthesis of 7-azaindolylcarboxy-endo-tropanamide (DF 1012). ORGANIC PROCESS RESEARCH & DEVELOPMENT, 7(2), 209-213.
Citazione: | Allegretti, M., Anacardio, R., Cesta, M.C., Curti, R., Mantovanini, M., Nano, G., et al. (2003). A practical synthesis of 7-azaindolylcarboxy-endo-tropanamide (DF 1012). ORGANIC PROCESS RESEARCH & DEVELOPMENT, 7(2), 209-213. | |
Tipo: | Articolo in rivista - Articolo scientifico | |
Carattere della pubblicazione: | Scientifica | |
Titolo: | A practical synthesis of 7-azaindolylcarboxy-endo-tropanamide (DF 1012) | |
Autori: | Allegretti, M; Anacardio, R; Cesta, MC; Curti, R; Mantovanini, M; Nano, G; Topai, A; Zampella, G | |
Autori: | ||
Data di pubblicazione: | mar-2003 | |
Lingua: | English | |
Rivista: | ORGANIC PROCESS RESEARCH & DEVELOPMENT | |
Appare nelle tipologie: | 01 - Articolo su rivista |