Aminothiazole derivatives, process for preparing them and pharmaceutical compositions containing them
申请人:——
公开号:US20020137740A1
公开(公告)日:2002-09-26
The subject of the invention is the compounds of formula:
1
in which R
1
, R
2
, R
3
, R
4
, R
5
and R
6
are as defined in Claim 1.
The compounds have a high affinity for the CRF receptors.
A new type of spirocyclic bisoxindole-based C2-symmetric diols (SBIDOLs) was designed and synthesized. A series of racemic SBIDOL derivatives (6a–6g) were readily synthesized from commercially available 2-halo-5-methoxyanilines 1 (X = Cl or Br) through N-mono alkylation, acylation, oxidation, double intramolecular Friedel–Crafts reaction, and demethylation reactions. The optical resolution of racemic