Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one useful in the preparation of the DPP-IV inhibitor (S)-1 ((2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7, 11b-hexahydro-2h-pyrido[2,1-a] isoquinolin-3-yl)-4-fluoromethyl-pyrrolidin-2-one
申请人:Abrecht Stefan
公开号:US20060270853A1
公开(公告)日:2006-11-30
This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula
and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula
which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.
PROCESS FOR THE PREPARATION OF (S)-4-FLUOROMETHYL-DIHYDRO-FURAN-2-ONE
申请人:Zutter Ulrich
公开号:US20080108816A1
公开(公告)日:2008-05-08
The present invention relates to a process of the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one of the formula
by employing a dialkylmalonate of the formula
wherein R
1b
is lower alkyl, and the use of this process for the manufacture of DPP-IV inhibitors that are useful for the treatment and/or prophylaxis of diseases such as diabetes.