An Efficient and Convenient Synthesis of 4,5,6,7-Tetrahydrothieno[3,2-c]pyridines by a Modified Pictet-Spengler Reaction via a Formyliminium Ion Intermediate
摘要:
A synthesis of N-formyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridines (5) was achieved in a highly efficient manner via trifluoroacetic acid catalyzed cyclization of formyliminium ion (4), which was produced by imination of 2-(2-thienyl)ethylamine (1) and a carbonyl compound (2) using titanium(IV) tetraisopropoxide followed by formylation with acetic-formic anhydride in a one-pot procedure. This modified Pictet-Spengler reaction provides a convenient method for preparing 4,5,6,7-tetahydrothieno[3,2-c]pyridines (6) possessing various substituents at C-4.
[EN] SUBSTITUTED SULFONAMIDE DERIVATIVES<br/>[FR] DÉRIVÉS SUBSTITUÉS DE SULFONAMIDE
申请人:GRUENENTHAL GMBH
公开号:WO2009124746A1
公开(公告)日:2009-10-15
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
这项发明涉及替代磺胺基衍生物,其制备方法,含有这些化合物的药物以及利用替代磺胺基衍生物制备药物。
Pyrazolopyrimidines, a process for their preparation and their use as medicine
申请人:Danysz Wojciech
公开号:US20080039476A1
公开(公告)日:2008-02-14
The invention relates to pyrazolopyrimidine derivatives of formula (I)
wherein
Y
1
, Y
2
and Y
3
independently are e.g. CR
10
, NH, S or O,
whereby at least one of Y
1
, Y
2
and Y
3
represents CR
10
;
R
1
represents chloro or bromo;
R
2
, R
3
, R
4
, R
5
, R
6
and R
7
represent e.g. hydrogen or C
1
-C
6
-alkyl, and
R
10
represents e.g. hydrogen, halogen or phenyl; which are potent mGluR5 modulators and are e.g. useful for the treatment of various neurological disorders.
Substituted sulfonamide compounds corresponding to formula I
processes for the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds for treating and/or inhibiting pain or other conditions at least partly mediated by the bradykinin 1 receptor.
6-halo-pyrazolo[1,5-a]pyridines, a process for their preparation and their use as metabotropic glutamate receptor (mGluR) modulators
申请人:Merz Pharma GmbH & Co. KGaA
公开号:EP2090576A1
公开(公告)日:2009-08-19
The invention relates to 6-halo-pyrazolo[1,5-a]pyridines of formula (I) as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.
wherein A represents -NR3R4
with R3 and R4 as described herein.