917027-02-2Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
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Page/Page column 88, (2013/04/13)
The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
A practical synthesis of optically active arylglycines via catalytic asymmetric Strecker reaction
Banphavichit, Vorawit,Mansawat, Woraluk,Bhanthumnavin, Worawan,Vilaivan, Tirayut
experimental part, p. 5849 - 5854 (2009/12/01)
A practical procedure for catalytic asymmetric synthesis of optically active arylglycine derivatives via optically active α-aminonitriles has been developed. The N-benzhydryl α-arylaminonitrile intermediates were prepared in excellent yield (89-99%) and enantiomeric purity (96 to >98% ee) by enantioselective cyanation of aldimines with TMSCN/iPrOH in the presence of 2.5 mol % of an easily prepared Ti/chiral amino alcohol complex at 0 °C, without requiring slow addition of the cyanating agent. The easily racemized α-aminonitrile intermediates were efficiently hydrolyzed by an aqueous HCl/TFA mixture to give the arylglycine derivatives in good yield (60-92%) and moderate to excellent enantiomeric purity (85-98% ee).
Chemo-enzymatic dynamic kinetic resolution of amino acid thioesters
Arosio, Dario,Caligiuri, Antonio,D'Arrigo, Paola,Pedrocchi-Fantoni, Giuseppe,Rossi, Cristina,Saraceno, Caterina,Servi, Stefano,Tessaro, Davide
, p. 1345 - 1348 (2008/09/16)
The L-forms of racemic-N-protected-β,γa,aunsaturated a-amino acid thioesters were found to be substrates for the subtilisin-catalysed hydrolysis to the corresponding acids. The D-enantiomer was continuously racemised in the presence of an organic base. The combined reactions in a biphasic system allowed the deracemisation of the amino acid derivatives based on a dynamic kinetic resolution. Excellent yields and enantioselectivities were achieved.
