83396-73-0Relevant academic research and scientific papers
HIV protease inhibitors and intermediates
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, (2008/06/13)
The present invention provides HIV protease inhibitors, intermediates for preparing HIV protease inhibitors. The enzyme, HIV protease, represents a viable target for the inhibition of HIV viral replication, thus providing a method for treating and/or prev
Asymmetric synthesis of L-thienylalanines
Meiwes, Johannes,Schudok, Manfred,Kretzschmar, Gerhard
, p. 527 - 536 (2007/10/03)
L-Thienylalanines were prepared via the hydantoin and azlactone routes with the key step consisting of the microbial transamination of 2-hydroxy-3-thienylacrylic with L-aspartic acid as amino donor.The transamination reaction was performed by a genetically engineered E. coli strain on scales up to 100 g of L-3-(2-thienyl)alanine 1a and is also applicable to the preparation of the isomeric amino acid 1b and some ring-substituted derivatives.
Protease inhibitors
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, (2008/06/13)
The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection.
UNUSUAL AMINO ACIDS. IV. ASYMMETRIC SYNTHESIS OF THIENYLALANINES
Doebler, Christian,Kreuzfeld, H.-J.,Krause, H. W.,Michalik, M.
, p. 1833 - 1842 (2007/10/02)
(Z)-2-N-Acylamino-3-thienyl-acrylic acids and thei esters were prepared by known procedures and hydrogenated to the corresponding optically active 2-N-acetyl(or benzoyl)-3-(2- or 3-thienyl)-alanines with optically yields up to 90percent using the rhodium complexes of 'PROPRAPHOS" 6a,b and O,N-bis(diphenylphosphino)-2-exo-hydroxy,3-endo-methylamino-norbornane 6c as chiral catalysts.Recrystallization and deacylation of the obtained amino acid derivatives yields the optically pure hydrochlorides of the thienylalanines as the free amino acids.
