[EN] QUINOLIZIDINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS<br/>[FR] MODULATEURS ALLOSTÉRIQUES POSITIFS DU RÉCEPTEUR M1 DE LA QUINOLIZIDINONE
申请人:MERCK & CO INC
公开号:WO2009051715A1
公开(公告)日:2009-04-23
The present invention is directed to spiropiperidine compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
A one-potsynthesis of diarylmethanes from air-stable diborylmethane via the Suzuki–Miyaura cross-coupling reaction is described. The present approach realizes the synthesis of various symmetrical and unsymmetrical diarylmethanes in good to excellent yields.
ROBERTS R. M.; EL-KHAWAGA AHMED M.; SWEENEY K. M.; EL-ZOHRY MAHER F., J. ORG. CHEM., 52,(1987) N 8, 1591-1599
作者:ROBERTS R. M.、 EL-KHAWAGA AHMED M.、 SWEENEY K. M.、 EL-ZOHRY MAHER F.
DOI:——
日期:——
Threefold and chemoselective couplings of triarylbismuths with benzylic chlorides and iodides using palladium catalysis
作者:Maddali L. N. Rao、Ritesh J. Dhanorkar
DOI:10.1039/c3ra46672h
日期:——
This paper describes the palladium-catalyzed studies on threefold coupling of triarylbismuth reagents with benzylic chlorides and iodides. The optimized protocol conditions are operationally simple, delivering threefold coupling of a variety of triarylbismuths in combination with benzylic chlorides and iodides. The two optimized protocols allowed the synthesis of a diverse range of unsymmetrical diarylmethanes in an efficient manner. As part of this study, chemoselective transformation of benzylic chlorides and iodides was also achieved.