公开(公告)号：EP2522656A2

公开(公告)日：2012-11-14

申请号：EP12160668.5

申请日：2004-07-23

申请人： REDX PHARMA LIMITED

发明人： Moody, David John ,  Wiffen, Jonathan William

IPC分类号： C07D207/34 ,  C07D309/30 ,  C07D405/06 ,  C07C231/02

CPC分类号： C07D405/06 ,  C07D207/34 ,  C07D309/10 ,  C07D309/30 ,  Y02P20/55

摘要： There is provided a process for the preparation of a compound of formula (7) or salts thereof:

wherein R 1 represents an alkyl group, R 2 represents an aryl group, R 3 represents an aryl group, and X represents a group of formula -COZ, wherein Z represents -OR 4 or NR 5 R 6 which comprises
a) cyanating a compound of formula (1) to give a compound of formula (2);
b) reducing 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) to give a compound of formula (5);
d) when W represents -OP 2 , deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6); and
e) subjecting the compound of formula (5) when W represents =O, or compound of formula (6) to ring-opening, and removal of any remaining protecting groups, to give a compound of formula (7) or salts thereof,
wherein the process comprises the further step of converting X from -COZ, wherein Z represents -OR 4 , to -COZ, wherein Z represents NR 5 R 6 , by reacting the compounds of formula (4), (5), (6) or (7) with a compound of formula HNR 5 R 6 ; and/or
wherein the process further comprises forming a compound of formuIa (2) or (3) wherein W represent =O by oxidising a compound of formula (2) or (3) when W represents -OP 2 and P 2 is hydrogen, or deprotecting and oxidising a compound of formula (2) or (3) when W represents -OP 2 and P 2 is a protecting group.

摘要翻译： 提供了制备式（7）化合物或其盐的方法：其中R 1表示烷基，R 2表示芳基，R 3表示芳基，X表示式 - COZ，其中Z表示-OR 4或NR 5 R 6，其包括a）将式（1）化合物氰化得到式（2）化合物; b）还原式（2）的化合物以得到式（3）的化合物; c）将式（3）化合物与式（4）化合物偶合得到式（5）化合物; d）当W代表-OP 2时，将式（5）化合物脱保护，然后氧化得到式（6）化合物; 以及e）当W代表= O时式（5）化合物或式（6）化合物开环，除去任何剩余的保护基团，得到式（7）化合物或其盐， 其中所述方法包括通过使式（4），（5），（6）的化合物与式（4）的化合物反应，将X从-COZ（其中Z表示-OR 4）转化为-COZ（其中Z表示NR 5 R 6） 或（7）与式HNR 5 R 6的化合物反应; 和/或其中所述方法还包括通过在W表示-OP 2且P 2为氢时，通过氧化式（2）或（3）的化合物形成式（2）或（3）的化合物，其中W表示= 或当W表示-OP 2且P 2为保护基时，使式（2）或（3）的化合物脱保护和氧化。

公开(公告)号：EP2522656A3

公开(公告)日：2013-03-20

申请号：EP12160668.5

申请日：2004-07-23

申请人： REDX PHARMA LIMITED

发明人： Moody, David John ,  Wiffen, Jonathan William

IPC分类号： C07D207/34 ,  C07D309/30 ,  C07D405/06 ,  C07C231/02

CPC分类号： C07D405/06 ,  C07D207/34 ,  C07D309/10 ,  C07D309/30 ,  Y02P20/55

摘要： There is provided a process for the preparation of a compound of formula (7) or salts thereof:

wherein R 1 represents an alkyl group, R 2 represents an aryl group, R 3 represents an aryl group, and X represents a group of formula -COZ, wherein Z represents -OR 4 or NR 5 R 6 which comprises
a) cyanating a compound of formula (1) to give a compound of formula (2);
b) reducing 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) to give a compound of formula (5);
d) when W represents -OP 2 , deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6); and
e) subjecting the compound of formula (5) when W represents =O, or compound of formula (6) to ring-opening, and removal of any remaining protecting groups, to give a compound of formula (7) or salts thereof,
wherein the process comprises the further step of converting X from -COZ, wherein Z represents -OR 4 , to -COZ, wherein Z represents NR 5 R 6 , by reacting the compounds of formula (4), (5), (6) or (7) with a compound of formula HNR 5 R 6 ; and/or
wherein the process further comprises forming a compound of formuIa (2) or (3) wherein W represent =O by oxidising a compound of formula (2) or (3) when W represents -OP 2 and P 2 is hydrogen, or deprotecting and oxidising a compound of formula (2) or (3) when W represents -OP 2 and P 2 is a protecting group.