Binuclear pyrazoles. I. Synthesis and cytotoxic activity of 1,1'-dibenzyl and 1,1'-dihydroxymethyl 4,4'-bispyrazoles.
Binuclear pyrazoles. I. Synthesis and cytotoxic activity of 1,1'-dibenzyl and 1,1'-dihydroxymethyl 4,4'-bispyrazoles.
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DOI：
10.1248/cpb.33.2535
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发表时间：
1985-06
影响因子：
1.7
通讯作者：
A. Cuadro;J. Elguero;P. Navarro
中科院分区：
文献类型：
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作者：
A. Cuadro;J. Elguero;P. Navarro
由3,3 ',5,5 '-四甲基- 4,4 '-双-1 h -吡唑、3,3 ',5,5 '-四甲基- 4,4 '-亚甲基-1 h -吡唑和4,4 '-亚甲基-1 h -吡唑得到相应的1,1 '-二苄基和1,1 '-二羟甲基衍生物。在相转移条件下，用氯化苄进行了1h -双吡唑的苄基化反应。用37%的甲醛水溶液在酸性或中性介质中进行羟甲基化。结果表明，1,1′-二苯基- 3,3′，5,5′-四甲基- 4,4′-双吡唑是一种强效细胞毒剂（ED50=7 μM）。
From 3, 3', 5, 5'-tetramethyl-4, 4'-bis-1 H-pyrazole, 3, 3', 5, 5'-tetramethyl-4, 4'-methylenebis-1 H-pyrazole and 4, 4'-methylenebis-1 H-pyrazole, the corresponding 1, 1'-dibenzyl and 1, 1'-dihydroxymethyl derivatives have been obtained. Benzylation of 1H-bispyrazoles was carried out by treatment with benzyl chloride under phase transfer conditions. Hydroxymethylation was done by treatment with 37% aqueous formaldehyde either in acidic or in neutral medium. All the products obtained have been evaluated as cytotoxic, and 1, 1'-dibenzyl-3, 3', 5, 5'-tetramethyl-4, 4'-bispyrazole is a powerful cytotoxic agent (ED50=7 μM).