| abstract |
The present invention provides a process of making N<1>,N4diethylspermine having the general formula: CH<7>CH<6>-N<1>H-(CH<6>)<7>-N<2>H-(CH<6>)<8>-N<3>H-(CH<6>)<7>-N4H-CH<6 >CH<7>. and pharmaceutically acceptable salts thereof by reacting spermine: N<1>H<6>-(CH<6>)<7>-N<2>H-(CH<6>)<8>-N<3>H-(CH<6>)<7>-N4H<6> with a sulfonating agent of the general formula RSO<6>X, where X stands for a leaving group and RSO<6> stands for a sulfonyl protecting group, e.g. an alkyl-, aralkyl- or aryl- sulfonyl protecting group, in the presence of a base, reacting the compound thus produced: <CHEM> with a strong base, e.g. NaH, and an ethylating agent in an aprotic dipolar solvent to produce a compound of the general formula: <CHEM> and removing the protecting groups under reducing conditions to provide N<1>,N4 diethylspermine, which optionally is converted into a pharmaceutically acceptable acid addition salt. |