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发明授权
CN1916009B 制备胺铂配合物的方法 失效 - 权利终止

制备胺铂配合物的方法
摘要：
本发明涉及铂药物领域。具体而言，本发明涉及一种制备通式(Ia)或(Ib)的铂配合物的改进方法，该方法包括：1a)第一步，其中，在适当的条件下，[PtA4]2-在第一溶剂中与L反应，形成[PtA3(L)]-；1b)第二步，其中，在适当的条件下，[PtA3(L)]-在第二溶剂中与L′反应，形成顺式-[PtA2(L′)(L)]；1c)Y是卤素或羟基的情况下的的第三步，其中，顺式-[PtA2(L′)(L)]与H2O2、含有Y2或卤素的氧化剂反应，形成c，t，c-[PtA2Y2(L′)(L)]；在Y是羧化物、氨基甲酸酯或碳酸酯的情况下的第四步，其中由步骤1c)形成的中间物，其中Y羟基，用适当的酰化剂官能化；和1d)在A不是卤根或者与原始卤根不同的情况下，需要此外加的步骤，在该步骤中，由步骤1a或1b、1c或1d形成的中间物的原始卤根A被转化为不同的卤根或者新的离去基团A，如单齿配位基羟基、烷氧基、羧化物或二齿配位基羧化物、膦酰基羧化物、二膦酸酯或硫酸酯；其中，L、L′和Y如说明书所述。
摘要（英）：

The present invention relates to the area of platinum drugs. In particular, it relates to an improved process for preparing platinum complexes having general formula (Ia) or (Ib), comprising: 1a) a first step, wherein [PtA4]<2-> is reacted with L under appropriate conditions in a first solvent to form [PtA3(L)]<->; 1b) a second step, wherein [PtA3(L)]<-> is reacted with L' under appropriate conditions in a second solvent to form cis-[(PtA2(L')(L)); 1c) in the case there Y is halogen or hydroxy a thrid step, wherein cis-[PtA<2>(L')(L)] is reacted with H2O2, Y2 or halogen containing oxidant to form c,t,c-[PtA2Y2(L')(L)]; in the case where Y is carboxylate, carbamate or carbonate ester a fourth step, wherein an intermediate, where Y is hydroxy formed in step 1c), is functionalized with an appropriate acylating agent; and 1d) in the case where A is not a halide or is different from the original halide, additional step(s) in which the original halide A of an intermediate formed in step 1a or 1b, 1c or 1d is converted to a different halide or a new leaving group(s) A such as mono-dentate hydroxy, alkoxy, carboxylate or bi-dentate carboxylate, phosphonocarboxylate, diphosphonate, or sulphate; wherein L, L' and Y have the meaning as defined in the description.

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