| 摘要 |
1520441 Di-(substituted alkyl)amino-benzenes CHEM PHARMAZ FABRIK DR HERMANN THIEMANN GmbH 11 July 1975 [16 July 1974] 29218/75 Heading C3H [Also in Division C2] Novel compounds I in which R1 is Y is N or N#O, each of X1 and X2 is H or C1-6 alkyl, X3 is halogen or C1-6 alkanesulphonyloxy, n is 0-6, R2 is C1-6 alkyl, R3 is OH (when n # 0), an alpha-amino acid residue or a polypeptide residue (when X1 is C1-6 alkyl or the group -NH-CH(R4)-COR5 (when X1 is H or C1-6 alkyl), where R4 is optionally substituted alkyl and R5 is OH (when n # 0), an alpha-aminoacid residue or a polypeptide residue, and esters and salts thereof, are prepared by hydroxyalkylating a compound II in which X is C1-6 alkyl, to convert the amino group into a di-(hydroxyalkyl)amino group, replacing the hydroxy groups by halogen atoms or alkanesulphonyloxy groups, if necessary after hydrolysis of the ester group to the carboxylic acid, followed by coupling a resultant carboxylic acid to an amino-acid or polypeptide or converting it to a salt or ester. Cytostatic compositions comprise a compound I together with a pharmaceutical carrier. |
