1489004-24-1Relevant articles and documents
An efficient catalytic asymmetric synthesis of a β2-amino acid on multikilogram scale
Remarchuk, Travis,Babu, Srinivasan,Stults, Jeffrey,Zanotti-Gerosa, Antonio,Roseblade, Stephen,Yang, Shaohui,Huang, Ping,Sha, Chunbo,Wang, Youchu
, p. 135 - 141 (2014)
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.
PROCESS FOR MAKING AMINO ACID COMPOUNDS
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, (2013/12/03)
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.
