PROCESSES FOR THE PREPARATION OF PYRIMIDINYLCYCLOPENTANE COMPOUNDS
The present invention relates to a process for the preparation of a compound of formula (I), wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
-
(2015/06/03)
An efficient catalytic asymmetric synthesis of a β2-amino acid on multikilogram scale
We describe herein a scalable catalytic asymmetric hydrogenation process for the multikilogram-scale production of a β 2-amino acid. A short and efficient synthesis of the starting unsaturated N-Boc-protected β 2-enamide was developed followed by extensive catalysis screening and optimization studies that identified a simple Ru-BINAP catalyst system to directly afford the (S) product in high enantiomeric excess and yield. The final process enabled the multikilogram production in >99% ee, to be used as a key component for one of our clinical candidates.
The invention provides new processes for making and purifying amino acid compounds, which are useful in the preparation of AKT inhibitors used in the treatment of diseases such as cancer, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.
-
(2013/12/03)
More Articles about upstream products of 1489004-27-4