Process for preparing caspofungin and intermediates thereof

Details Process for preparing caspofungin and intermediates thereof Process for preparing caspofungin and intermediates thereof

C - Chemistry, Metallurgy

07

K

C07K 7/54 (2006.01)

Patent

CA 2727567

The present invention relates to novel intermediates of formula (VII), or an acid addition salt or a solvate thereof, wherein R, is -(CO)NH2, -CH2NH2 or -CN; R2 = R3 = H or R2 and R3 together form a cyclic boronate or borate ester; X is a helping group selected from the group consisting of i) a five or six membered heterocyclic aromatic ring and derivatives thereof comprising at least one N-atom being a part of an imine-group, wherein said N-atom forms the point of connection to the cyclohexapeptide ring, and ii) tetrazolyl and derivatives thereof for which a nitrogen atom forms the point of connection to the cyclohexapeptide ring, and a process for the preparation of caspofungin utilizing said intermediates.

La présente invention concerne de nouveaux intermédiaires de formule (VII), ou un sel daddition acide ou un solvate correspondant; dans cette formule, R1 est -(CO)NH2, -CH2NH2 ou -CN; R2 = R3 = H ou R2 et R3 forment ensemble un boronate cyclique ou un ester de borate; X est un groupe aidant choisi dans le groupe constitué de i) un cycle aromatique hétérocyclique à cinq ou six éléments et des dérivés correspondants renfermant au moins un atome N faisant partie dun groupe imine, ledit atome N constituant le point de connexion au cycle cyclohexapeptide, et ii) du tétrazolyle et des dérivés correspondants pour lesquels un atome dazote constitue le point de connexion au cycle cyclohexapeptide, et un processus de préparation de caspofungine utilisant lesdits intermédiaires.

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