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Title:
PREPARATION OF 2-ACYL-2,5-DIHYDROXY-1,2,3,4-TETRA-HYDRONAPHTHACENE-6,11-DI ONE DERIVATIVE
Document Type and Number:
Japanese Patent JPS61100545
Kind Code:
A
Abstract:

PURPOSE: To produce the titled compound useful as a synthetic intermediate of a compound having carcinostatic activity, with simple reaction operation, in high yield, by reacting a specific carboxylic acid derivative with a specific carbonyl compound, and reacting the reaction product with a Grignard reagent.

CONSTITUTION: The objective compound of formula IV useful as a synthetic intermediate of the compound of formula III (X is R) which is an aglicon of a non-natural anthracycline exhibiting excellent carcinostatic activity, is produced by (1) reacting the 2, 5-dihydroxy-1,2,3,4-tetrahydronaphthacene-6,11-dione-2- carb-oxylic acid derivative of formula I (R is H or OH) with the carbonyl compound of formula II (A and A' are azole group) such as 1,1'- carbonyldiimidazole, etc. in a solvent, and (2) reacting the obtained reaction mixture with a Grignard reagent of formula R1MgX (R1 is alkyl, aralkyl or aryl; X is halogen) in the presence of a Lewis acid. When an optically active compound is used as the raw material, it can be converted to the optically active compound having the corresponding absolute configuration without causing the racemization.


Inventors:
TERAJIMA ATSURO
KIMURA YOSHIICHI
MATSUMOTO MITSUYO
SUZUKI MICHIYO
ABE RUMIKO
Application Number:
JP22221684A
Publication Date:
May 19, 1986
Filing Date:
October 24, 1984
Export Citation:
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Assignee:
SAGAMI CHEM RES
International Classes:
C07C50/38; C07C45/00; C07C46/00; C07C67/00; (IPC1-7): C07C46/00; C07C50/38



 
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