Process for producing (amido)n-substituted bleomycins

Details Process for producing (amido)n-substituted bleomycins Process for producing (amido)n-substituted bleomycins

C - Chemistry, Metallurgy

07

K

530/9

C07K 9/00 (2006.01) A61K 31/16 (2006.01) A61K 31/41 (2006.01) C07D 417/02 (2006.01) C07D 417/04 (2006.01) C07H 15/26 (2006.01) C07K 5/02 (2006.01) C12P 19/58 (2006.01)

Patent

CA 1276400

ABSTRACT OF THE DISCLOSURE A process for producing (amido)N-substituted bleomycins represented by the general formula Image wherein BM is a residue of bleomycin skelton, X is a C1 to C10 alkyl group which may be substituted by a C1 to C4 alkyl-amino, di(C1 to C6 alkyl) amino or N-[(C1 to C4 alkyl)amino-C1 to C4 alkyl]N-C1 to C4 alkylamino group, wherein the alkyl substituent may have a phenyl substituent, which phenyl may be substituted with a halogen atom; R1 is (1) a cycloalkyl group having 6 to 10 carbon atoms, (2) a C1 to C4 alkyl group having a phenyl substituent (the phenyl may further have a halogen substituent), or (3) a phenyl group which may have one or more substituents selected from halogen atoms, cyano and benzyloxy, and R2 is a halogen atom or -CH2-R1, wherein R1 is as defined above, which comprises allowing an (amindo)N-substituted derivative represented by the general formula Image wherein BM has the same definition as above and X is an alkyl group which may have substituents, to condense reductively with an aldehyde represented by the general formula R1CHO wherein R1 has the same definition as above.

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