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antimitotic derivatives of vinca alkaloids, process for preparing them and use of the derivatives.
antimitotic derivatives of vinca alkaloids, process for preparing them and use of the derivatives.
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机译:长春花生物碱的抗有丝分裂衍生物,其制备方法和衍生物的用途。
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摘要
Antimitotic Vinca alkaloid derivatives of formula (I), their salts with acids, and their diastereoisomers and mixtures, and processes for their preparation are new. In formula (I), n = 1 or 2, R1 = H or F; R2 = Cl. Process for the preparation of vinflunine (I; n = 2; R1 = H; R2 = difluoro), by reaction of (II) in a superacid medium (HF + SbF5) at -45 to -35 deg C, with a halide generator (chloroform, 2,2-dichloropropane, carbon tetrabromide, dibromomethane, or boron tribromide) is also claimed, where R3 = OH; R4 = H, or R3 and R4 together form a double bond.
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