METHOD FOR THE SYNTHESIS OF CLOFARABINE

Method for the production of the anticancer nucleoside clofarabine in high yield, the method comprising the preparation of 2- chloroadenosine by enzymatic transglycosylation between 2- chloroadenine and nucleosides, benzoylation, isomerization, sulfonate ester formation, fluorination, and deprotecti...

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Hauptverfasser: MATVIENKO, VICTOR, SYPCHENKO, VOLODYMYR, ZABUDKIN, ALEXANDER, MATVIIENKO, IAROSLAV
Format: Patent
Sprache:eng ; fre
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Zusammenfassung:Method for the production of the anticancer nucleoside clofarabine in high yield, the method comprising the preparation of 2- chloroadenosine by enzymatic transglycosylation between 2- chloroadenine and nucleosides, benzoylation, isomerization, sulfonate ester formation, fluorination, and deprotection. On décrit un procédé de production à rendement élevé de la clofarabine, un analogue nucléosidique anticancéreux. Le procédé consiste à préparer 2-chloroadénosine par: transglycosylation enzymatique entre 2-chloroadénine et des nucléosides, benzoylation, isomérisation, formation d'ester de sulfonate, fluoration et déprotection.