Synthesis of Antitumor Pyridine and Pyridazine N-Oxides having (2-Chloroethyl) nitrosoureidomethyl and Bis (2-chloroethyl)-aminomethyl Groups
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概要
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Treatment of 1-(2-chloroethyl)-1-nitroso-3-(3-pyridylmethyl) urea (Ia) and the 3-nitroso isomer (Ib) with m-chloroperbenzoic acid, gave the corresponding N-oxides, IIa and IIb. The 3-nitrosoureas (Ib, IIb) isomerized to the 1-nitroso isomers (Ia, IIa) by dissolving them in formic acid. The reaction of 6-bis (2-chloroethyl) aminomethyl-3-hydroxypyridazine 1-oxide (III) with bromine gave the 4-bromo derivative (IV). 1-(2-Chloroethyl)-1-nitroso-3-(3-pyridylmethyl) urea N-oxide (IIa) showed the most marked activity against rat ascites hepatom AH-13 and mouse lymphoid leukemia L-1210.
- 公益社団法人日本薬学会の論文
- 1978-12-25
著者
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神谷 庄造
National Institute of Hygienic Sciences, University of Tokyo
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鈴木 郁生
国立衛生試験所
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鈴木 郁生
National Hygienic Laboratory
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宮原 美知子
国立医薬品食品衛生研究所 衛生微生物部
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宮原 美知子
National Institute of Hygienic Sciences
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末吉 祥子
National Institute of Hygienic Sciences
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小田嶋 成和
National Institute of Hygienic Sciences
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神谷 庄造
National Institute Of Hygienic Sciences
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