公开(公告)号：EP3356332A1

公开(公告)日：2018-08-08

申请号：EP16852356.1

申请日：2016-09-26

申请人： Merck Sharp & Dohme Corp. ,  Merck Sharp & Dohme Limited

发明人： CHEN, Qinghao ,  SCOTT, Jeremy ,  KRSKA, Shane, W. ,  BAXTER, Carl ,  STEWART, Gavin William ,  TAN, Lushi ,  GIBB, Andrew ,  MALIGRES, Peter, E.

IPC分类号： C07D239/70 ,  A61K31/517 ,  A61P25/28 ,  C07D401/10

CPC分类号： C07D401/06 ,  A61K31/517

摘要： This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.

公开(公告)号：EP2725905A1

公开(公告)日：2014-05-07

申请号：EP12804259.5

申请日：2012-06-25

申请人： Merck Sharp & Dohme Corp. ,  Merck Sharp & Dohme Limited

发明人： TAN, Lushi ,  CHEN, Qinghao ,  ZACUTO, Michael, J. ,  DUNN, Robert, F. ,  MOMENT, Aaron, J. ,  JANEY, Jacob, M. ,  LIEBERMAN, David ,  SHEEN, Faye ,  BREMEYER, Nadine ,  SCOTT, Jeremy ,  KUETHE, Jeffrey, T.

IPC分类号： A01N43/56

CPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/513 ,  C07B2200/13 ,  Y02P20/55

摘要： A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.