Novel intermediates useful for the preparation of antihistaminic piperidine derivatives
申请人:Merrell Pharmaceuticals Inc.
公开号:US20010020114A1
公开(公告)日:2001-09-06
The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula
1
wherein
W represents —C(═O)— or —CH(OH)—;
R
1
represents hydrogen or hydroxy;
R
2
represents hydrogen;
R
1
and R
2
taken together form a second bond between the carbon atoms bearing R
1
and R
2
;
n is an integer of from 1 to 5;
m is an integer 0 or 1;
R
3
is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy: and
pharmaceutically acceptable salts and individual optical isomers thereof,
with the proviso that where R
1
and R
2
are ta to form a second bond between the carbon t
R
1
and R
2
or where R
1
represented hydroy&ggr; integer 0.
本发明涉及一种新型中间体和过程,其在制备某些抗组胺哌啶衍生物的过程中有用,该衍生物的化学式为1,其中W代表—C(═O)—或—CH(OH)—;R1代表氢或羟基;R2代表氢;R1和R2共同形成连接R1和R2所在碳原子之间的第二键;n为1至5的整数;m为0或1的整数;R3为—COOH或—COOalkyl,其中烷基部分具有1至6个碳原子,直链或支链,每个A均为氢或羟基;以及药学上可接受的盐和各自的光学异构体,但其中R1和R2共同形成连接R1和R2所在碳原子之间的第二键,或R1代表羟基时,m为0。