| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new chain polyamine compound having carcinostatic action and useful as an active component for anticancer agent. SOLUTION: The objective compound is expressed by formula I [(n) is 1-8; R1 and R3 are each H or p-toluenesulfonyl; R2 and R4 are each ethyl or group of formula II ((m) is 1 or 2; R5 is H or p-toluenesulfonyl; R6 is H, ethyl, an aldehyde or cyclopropylmethyl or R5 and R6 together form a phthaloyl group)], e.g. 1,18-bis(ethylamino)-5,14-azaoctadecane. The compound of formula I is produced by reacting a compound of formula III with N2H2, reacting the produced compound in 2N-HCl and further reacting with TsCl in the presence of pyridine and NEt3 to obtain a tosylamide derivative of formula IV. In the case of introducing ethyl group, the product is reacted with a mixture of Et-Br and K2CO3. A detosylated compound can be produced by treating with 33% HBr-AcOH (acetic acid).
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