105198-42-3Relevant articles and documents
ASPARAGINE DERIVATIVES AND METHODS OF USE THEREOF
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Paragraph 001027; 001029-001030, (2021/12/31)
The present invention relates to compounds of formulas (A) and (I), pharmaceutically acceptable salts thereof, and solvates of any of them, pharmaceutical compositions comprising them, methods of preparation thereof, intermediate compounds useful for the preparation thereof, and methods of treatment or prophylaxis of diseases, in particular cancer, such as colorectal cancer, using these. (A) (I)
Enantioselective synthesis of allylboronates bearing a tertiary or quaternary B-substituted stereogenic carbon by NHC-Cu-catalyzed substitution reactions
Guzman-Martinez, Aikomari,Hoveyda, Amir H.
supporting information; scheme or table, p. 10634 - 10637 (2010/11/05)
Allylic substitutions that afford α-substituted allylboronates bearing B-substituted tertiary or quaternary carbon stereogenic centers are presented. C-B bond-forming reactions, catalyzed by chiral bidentate Cu-NHC complexes, are performed in the presence of commercially available bis(pinacolato)diboron. Transformations proceed in high yield (up to >98%) and site selectivity (>98% SN2′), and in up to >99:1 enantiomer ratio. Trans- or cis-disubstituted alkenes can be used; alkyl- (linear as well as branched) and aryl-trisubstituted allylic carbonates serve as effective substrates. Allylboronates that bear a quaternary carbon center are air-stable and can be easily purified by silica gel chromatography; in contrast, secondary allylboronates cannot be purified in the same manner and are significantly less stable. Oxidation of the enantiomerically enriched products furnishes secondary or tertiary allylic alcohols, valuable small molecules that cannot be easily obtained in high enantiomeric purity by alternative synthesis or kinetic resolution approaches.
Practical synthesis of Abbott amino-diol: A core unit of the potent renin inhibitor Zankiren
Chandrasekhar,Mohapatra, Suchismita,Yadav
, p. 4763 - 4768 (2007/10/03)
Abbott amino-diol (2S,3R,4S)-2-amino-1-cyclohexyl-6-methyl heptane-3,4- diol 1, a main structural constituent of the orally active renin inhibitor Zankiren has been synthesized using Sharpless asymmetric aminohydroxylation as the key step.