| 摘要 |
<p>There are provided new antitumor salts of oxazaphosphorine derivatives of the formula <IMAGE> where R1, R2, and R3 are the same or different and represent hydrogen, methyl, ethyl, 2-chloroethyl, or 2-methanesulfonyloxyethyl and wherein at least two of these residues are 2-chloroethyl and/or 2-methanesulfonyl-oxyethyl and A is the group -S-alk-SO3H or -N(OH)-CONH-alk-CO2H and alk represents a C2-C6-alkylene residue optionally containing a mercapto group, whereby alk also can be -CH2- in case there is a carboxy group attached to the alk group, with homocysteinethiolactone or alpha -amino- epsilon -caprolactam or a basic compound of the formula: <IMAGE> II wherein R4 is a hydroxy group, an amino group or a C1-C6-alkoxy group, R5 is hydrogen or a difluoromethyl group, R6 is hydrogen, an indolyl-(3)-methyl residue, imidazolyl-(4)-methyl residue, a C1-C10-alkyl group or a C1-C10-alkyl group which is substituted by a hydroxy group, a C1-C6-alkoxy group, a mercapto group, a C1-C6-alkylmercapto group, a phenyl group, a hydroxy phenyl group, an amino-C1-C6-alkylmercapto group, an amino-C1-C6-alkoxy group, an amino group, an aminocarbonyl group, a ureido group (H2NCONH-), a guanidino group or a C1-C6-alkoxycarbonyl group, or wherein R6 together with the structured portion >CR5(NR7R8) forms the proline residue, the 4-hydroxy-proline residue or the 2-oxo-3-amino-3-difluoromethyl-piperidine and the residues R7 and R8 represent hydrogen or C1-C6-alkyl residues.</p> |
