916069-80-2Relevant articles and documents
Development of a scalable synthesis of (S)-3-fluoromethyl-γ- butyrolactone, building block for Carmegliptin's Lactam moiety
Adam, Jean-Michel,Foricher, Joseph,Hanlon, Steven,Lohri, Bruno,Moine, Gerard,Schmid, Rudolf,Wirz, Beat,Zutter, Ulrich,Stahr, Helmut,Weber, Martin
experimental part, p. 515 - 526 (2011/12/05)
Several new routes are reported for the synthesis of (S)-3-fluoromethyl- γ-butyrolactone. An asymmetric hydrogenation-based synthesis was chosen as the enabling route to produce the lactone on a 10-kg scale. A superior stereoselective route starting from (S)-tert-butyl glycidyl ether which afforded the desired lactone in three steps with ~50% overall yield was finally selected for further development and production.
PROCESS FOR THE PREPARATION OF (S)-4-FLUOROMETHYL-DIHYDRO-FURAN-2-ONE
-
Page/Page column 9; 9-10, (2008/12/04)
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 R1b 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.
PROCESS FOR THE PREPARATION OF PYRIDO [ 2-1-A] ISOQUINOLINE DERIVATIVES BY CATALYTIC ASYMMETRIC HYDROGENATION OF AN ENAMINE
-
Page/Page column 20, (2008/06/13)
The invention relates to a process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the formula wherein R2, R3and R4 are as defined in the specification, comprising the steps of a) catalytic asymmetric hydr