NOVEL 4-DEOXYDAUNOSAMINE ANALOGUE, PREPARATION THEREOF, ANTHRACYCLINE OBTAINED BY USING THESE ANALOGUE AND USE OF ANTHRACYCLINE AS DRUG

Japanese Patent JPH02196779

A

NEW MATERIAL: A compd. represented by formula I (one of R1 and R2 is OH, alkoxy or acyloxy and the other is H, and when R2 is H, an α-stereoisomer is obtained and, when R1 is H, a β-stereoisomer is obtained; R3 is H or COR4; R4 is R6 or perfluoroalkyl; R6 is substd. or non-substd. alkyl or aryl).

EXAMPLE: 3-N-trifluoroacetylaminomethyl-2,3,4,6-tetradeoxy-L-lyxohexopyranose.

USE: An intermediate of novel anthracycline having cytotoxity and stability high in treatment effect at a cancer drug.

PROCESS: A compd. represented by formula 10 obtained by reducing a compd. represented by formula 8a is treated with a compd. represented by formula CF3COOR5 (R5 is alkyl) and, subsequently, an acetal group is hydrolyzed if desired and, further, an alcohol group is esterified if desired to obtain compds. Ia-Ic. These compds. can be derived to novel substances represented by formula 2 by the acid catalyst reaction with anthracyclinones.

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BURIJITSUTO RUNUU
JIYANNPIEERU JIESON
JIYANNKUROODO JIYAKUSHI
HANSU PEETAA KUREEMAA

JP25171589A

August 03, 1990

September 27, 1989

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RABO HOECHST SA
BEHRINGWERKE AG

A61K31/65; A61P35/00; C07C255/13; C07D309/10; C07D309/12; C07H15/252; (IPC1-7): A61K31/65; C07C255/13; C07D309/10; C07D309/12

Michio Nakajima (2 outside)

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