Method for preparing echinocandin derivatives and their compositions

Disclosed is a process for the preparation of a compound of formula (I), wherein R is a cyclic chain optionally containing heteroatoms and heterocycles, the process comprising: (a) acylating a compound of formula (II) with an acid of formula R-CO2H, wherein the acid is optionally in an isolated or n...

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Hauptverfasser: COLLADANT, COLETTE, DROUX, SERGE, LEMAITRE, GUY, BOFFELLI, PHILIPPE, ELTER, MICHEL, FERROUD, DIDIER, BROUILLARD, AGNES, PALADINO, JOSEPH
Format: Patent
Sprache:eng
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Zusammenfassung:Disclosed is a process for the preparation of a compound of formula (I), wherein R is a cyclic chain optionally containing heteroatoms and heterocycles, the process comprising: (a) acylating a compound of formula (II) with an acid of formula R-CO2H, wherein the acid is optionally in an isolated or non-isolated, activated form, to obtain a compound of formula (III), (b) optionally alkylating the alcohol in position 5 of the compound of formula (III) with an alcohol of formula Alk-OH, in the presence of PPTS, to obtain a compound of formula (IIIÆ), (c) dehydrating the compound of formula (III) or (IIIÆ), to obtain a compound of formula (IV), (d) reductively aminating the compound of formula (IV) with ethylene diamine in the presence of a reducing agent, to obtain a compound of formula (I).