4-Desacetyl VLB C-3 carboxhydrazides, their preparation and formulations containing them
申请人:ELI LILLY AND COMPANY
公开号:EP0005051A1
公开(公告)日:1979-10-31
4-Desacetyl vincaleucoblastine C-3 carboxhydrazides of the formula
wherein Q is
R is, when taken singly, C1-C3 alkyl, β-hydroxyethyl, β-acetoxyethyl, C2-C4 alkanoyl, dichloroacetyl, benzoyl or C1-C3 alkyl carbazyl;
R1 is, when taken singly, methyl or H only when R is C1-C3 alkyl and is H otherwise; and
R and R', when taken together, form a C1-C3 alkylidene group.
The compounds are prepared by reacting the C-3 carboxazides with
or by reacting the unsubstituted C-3 carboxhydrazide with acetone or with the appropriate aldehyde, acid anhydride or acid chloride.
The compounds are useful in inhibiting the growth of tumors.
式中的 4-去乙酰基长春花碱 C-3 羧酰肼
其中 Q 是
R单个时为C1-C3烷基、β-羟乙基、β-乙酰氧乙基、C2-C4烷酰基、二氯乙酰基、苯甲酰基或C1-C3烷基苄基;
R1 单个时为甲基,或仅当 R 为 C1-C3 烷基时为 H,否则为 H;以及
R 和 R'合在一起时形成一个 C1-C3 亚烷基。
这些化合物的制备方法是将 C-3 羧氮化物与
或未取代的 C-3 羧酰肼与丙酮或适当的醛、酸酐或酸氯化物反应。
这些化合物可用于抑制肿瘤的生长。