[EN] PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS, PARTICULARLY ROSUVASTATIN<br/>[FR] PROCEDE ET COMPOSES INTERMEDIAIRES UTILES DANS LA PREPARATION DE STATINES ET PLUS SPECIFIQUEMENT DE ROSUVASTATINE
申请人:AVECIA PHARMACEUTICALS LTD
公开号:WO2005092867A2
公开(公告)日:2005-10-06
There is provided a process for the preparation of a compound of formula (7) wherein R1 represents an alkyl group; R2 represents an aryl group; R3 represents hydrogen, a protecting group or an alkyl group; and R4 represents hydrogen, a protecting group or a SO2R5 group where R5 is an alkyl group, which comprises a) hydroxylating a compound of formula (1) wherein Y represents a halo group; P1 represents hydrogen or a protecting group, and W represents =O or -OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2), b) oxidising the compound of formula (2) to give a compound of formula (3), c) coupling the compound of formula (3) with a compound of formula (4), wherein R3 represents a protecting group or an alkyl group; R4 represents a protecting group or a SO2R5 group where R5 is an alkyl group; and R6 represents (PR7R8)+X- or P(=O)R7R8 in which X is an anion and R7 and R8 each independently is an alkyl, aryl.
提供了一种制备化合物的方法,该化合物的化学式为(7),其中R1代表烷基;R2代表芳基;R3代表氢原子、保护基或烷基;R4代表氢原子、保护基或SO2R5基团,其中R5代表烷基。该方法包括:a)对化学式(1)的化合物进行羟基化反应,其中Y代表卤素基团;P1代表氢原子或保护基;W代表=O或-OP2,其中P2代表氢原子或保护基,得到化合物的化学式(2);b)将化合物的化学式(2)进行氧化反应,得到化合物的化学式(3);c)将化学式(3)的化合物与化学式(4)的化合物偶联,其中R3代表保护基或烷基;R4代表保护基或SO2R5基团,其中R5代表烷基;R6代表(PR7R8)+X-或P(=O)R7R8,其中X是阴离子,R7和R8各自独立地代表烷基或芳基。