申请人:Fresenius Kabi Oncology Limited
公开号:US07608730B2
公开(公告)日:2009-10-27
We disclose here processes for making Platinum complex of general formula (I) where in, the conformation of 1,2-diaminocyclohexane is cis, trans-l or trans-d isomer and R1 and R2 combinedly make dicarboxylic acid having formulae (II), (III) and (IV), here in, the two carboxylic acid groups are on the same or on vicinal carbon atoms, n is zero or an integer ranging from 1 to 5 and R3 is either hydrogen or a substituent with electron withdrawing or electron releasing effects exemplified by alkoxy, halo, and nitro groups by reacting a compound of formula M2PtX4 wherein X represents halogen atom such as Cl or Br or thiocyanate with (i) 1,2-diaminocyclohexane (ii) source of silver ion selected from a silver compound containing divalent anion in presence of a corresponding carboxylic acid of formula (II) or (III) or (IV) to get the compound of formula (I), purifying the said compound by treating with alkali metal iodide and isolating the title compound by any conventional methods. The preparation of the said compound involves, for the first time, the intermediate formation of cis-Diiodo-trans-l-1,2-diaminocyclohexane platinum(II) and biscarboylato-trans-l-1,2-diaminocyclohexane platinum(II).
我们在这里披露了制备一般式(I)的铂配合物的过程,其中1,2-二氨基环己烷的构象为顺式、反式-l或反式-d异构体,R1和R2结合形成具有公式(II)、(III)和(IV)的二羧酸,其中两个羧酸基在同一碳原子上或相邻的碳原子上,n为0或1至5的整数,R3为氢或具有电子吸引或电子释放效应的取代基,例如烷氧基、卤素和硝基基团,通过将化合物M2PtX4(其中X代表卤素原子,例如Cl或Br或硫氰酸根)与(i)1,2-二氨基环己烷和(ii)选择性地含有二价阴离子的银化合物源,在相应的羧酸(II)或(III)或(IV)存在下反应,得到公式(I)的化合物,通过用碱金属碘化物处理所述化合物来纯化所述化合物,并通过任何常规方法分离所述化合物。所述化合物的制备首次涉及顺-二碘-反-l-1,2-二氨基环己烷铂(II)和双羧酸基-反-l-1,2-二氨基环己烷铂(II)的中间体形成。