Process of preparing etoposide phosphate and etoposide

Details Process of preparing etoposide phosphate and etoposide Process of preparing etoposide phosphate and etoposide

C - Chemistry, Metallurgy

12

P

C12P 19/60 (2006.01) C07F 9/547 (2006.01) C07H 15/18 (2006.01) C07H 15/24 (2006.01) C07H 15/26 (2006.01) C07H 17/04 (2006.01)

Patent

CA 2133594

Etoposide phosphate is prepared by coupling dibenzyl 4'-demethyl-4-epipodophyllotoxin-4'-phosphate with 2,3-di-O-benzyl-4,6-0-ethylidene-a,.beta.-D-glucopyranose in a solvent and subsequently removing the protecting groups. The tetra-benzyl protected etoposide phosphate is recrystallized from methanol or directly crystallized from acetonitrile by adding methanol to yield substantially the pure C-1"-.beta. form. The benzyl protecting groups are simultaneously removed by hydrogenation to produce etoposide phosphate in high yields. In a further embodiment, etoposide phosphate is treated with a phosphatase enzyme to yield etoposide.

On prépare de l'étoposide-phosphate en couplant du dibenzyl-4'-déméthyl-4-épipodophyllotoxine-4'-phosphate avec du 2,3-dibenzyl-4,6-O-éthylidène-.alpha.,.bêta.-D-glucopyrannose dans un solvant et en éliminant ultérieurement les groupes protecteurs. L'étoposide-phosphate protégé par quatre groupements benzyles est recristallisé à partir de méthanol ou directement cristallisé à partir d'acétonitrile en ajoutant du méthanol, afin de produire principalement la forme C-1"-.bêta. pure. Les groupements protecteurs benzyles sont éliminés simultanément par hydrogénation pour produire de l'étoposide-phosphate avec un rendement élevé. Dans une autre application, l'étoposide-phosphate est traité avec une phosphatase afin de produire de l'étoposide.

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