Derivatives of morpholinyl daunorubicin and morpholinyl...

Details Derivatives of morpholinyl daunorubicin and morpholinyl... Derivatives of morpholinyl daunorubicin and morpholinyl...

C - Chemistry, Metallurgy

07

H

260/208.1

C07H 15/252 (2006.01)

Patent

CA 1239396

Abstract of the Disclosure A group of new daunorubicin and doxorubicin derivatives having antitumor activity of the structure : Image wherein R is -CO-CH3 or -CHOH-CH3, -CO-CH2OH or -CHOH-CH2OH; hydroxy; a 1 to 3 carbon alkyl; a 1 to 3 carbon terminal hydroxyalkyl; 2 to 7 carbon organic acid-based esters and diesters of -CO-CH2OH, -CHOH-CH2OH, and -CHOH-CH3, and 13-ketimine derivatives of -CO-CH3 or -CO-CH2OH; Y is usually methoxy (-OCH3) but can also be hydrogen, X is =O or =NH; R' and R" together are a hydrogen and a hydroxy (that is, either R' or R" is hydroxy with the other hydrogen, both are hydrogens or R' is methoxy and R" is hydrogen), and A is selected from cyano (-C?N) and hydrogen as set forth above. Z is selected from oxygen sulfur, Image wherein R''' is a 1 to 3 carbon alkyl, and -CH2- subject to the proviso that when Z is -CH2- or Image , A is -C-N. Suitable process for the preparation of the compounds which are antitumor agents is also described.

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