Title:
PRODUCTION OF ETOPOSIDES
Document Type and Number:
Japanese Patent JP3904269
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To produce etoposides in high yield, reducing a formation of a by- product and without using a harmful halogen-based solvent by using a specific amount of a specified non-halogen-based solvent when a protected demethyl- epipodophyllotoxin is reacted with a protected glucose derivative.
SOLUTION: A protected 4'-demethyl-4-epipodophyllotoxin of formula I (R1 is a protection group of a hydroxy group) is reacted with a glucose derivative of formula II (R2 is a protection group of a hydroxy group) in a non-halogen- based solvent containing 0.1-7 times vol.pts. of a non-halogenated aliphatic solvent based on the compound of formula I in the presence of a dehydrating catalyst (preferably a complex of boron trifluoride and diethyl ether, etc.) preferably at -5 to -20°C to provide etoposides of formula III, having protected function groups. The protected product is, if necessary, deprotected. Acetonitrile is preferable as the non-halogenated aliphatic solvent. The use of a mixed solvent of the non-halogenated aliphatic solvent with a non-halogenated aromatic solvent is preferable in the point of reducing the by-product formation.
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Inventors:
Yukihiro Fusauchi
Yoshikawa hiro
Yoshikawa hiro
Application Number:
JP33629696A
Publication Date:
April 11, 2007
Filing Date:
December 03, 1996
Export Citation:
Assignee:
NIPPON KAYAKU KABUSHIKI KAISHA
International Classes:
C07H1/00; C07H17/04; A61K31/70; A61K31/7042; A61K31/7048; A61P35/00; C07B61/00; (IPC1-7): C07H17/04; C07H1/00; //A61K31/70; C07B61/00; C07M7:00
Domestic Patent References:
| JP7196680A | ||||
| JP5178880A | ||||
| JP5306293A | ||||
| JP2295996A | ||||
| JP63028438B1 | ||||
| JP6509334A |