5-Fluoro-and 5-chlorocyclophosphamide: synthesis, metabolism, and antitumor activity of the cis and trans isomers

…, M Jarman, RW Kinas, JMS Van Maanen…

文献索引：Foster; Jarman; Kinas; van Maanen; Taylor; Gaston; Parkin; Richardson Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1399 - 1403

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被引用次数: 17

摘要

In seeking analogues of cyclophosphamide (1) having improved antitumor activity by virtue of accelerated formation of the cytotoxic metabolite phosphoramide mustard, cis and trans isomers of 5-fluoro-and 5-chlorocyclophosphamide (9, 10, 11 and 12, respectively) were synthesized by condensation of the appropriate 3-amino-2-halopropan-1-01 (13 or 26) with N, N-bis (2-chloroethyl) phosphoramidic dichloride (14). The metabolism of the ...