| 摘要 |
Gem-dihalo and -tetrahalo-1, 12-diamino-4, 9-diaza dodecane derivs. of formula (I) and salts are prepd.. In the formula, X and Y are each H or halo, if dihalo cpds. have halo on only one C atom and tetrahalo derivs. are 2,2,11,11-halo-substd. Esp. cpds. may be prepd. from 2,2- dihalo-1,4-butane diols e.g. by reaction with MeSO3Cl to 1,4-bis- methane-sulphonyloxy-2,2-dihalo butane conversion to corresp. diphthalimido cpds., hydrazine treatment to corresp. diamino diamino butanes, protection and alkylation to 4,9-diaza dodecanes and deprotection. (I) are spermine derivs. which antagonise spermine functions in cell and so are antiproliferation and antitumour agents.
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