148205-40-7Relevant academic research and scientific papers
Asymmetric α-Allylation of α-Substituted β-Ketoesters with Allyl Alcohols
Yoshida, Masanori
, p. 12821 - 12826 (2017/12/08)
Enantioselective α-allylation of α-substituted β-ketoesters with simple allyl alcohols was successfully performed by synergistic catalysis with the catalyst combination of a chiral primary amino acid and an achiral palladium complex without additional promotors like acids or bases. The allylation reaction and generation of a chiral quaternary carbon stereocenter proceeded smoothly to produce α,α-disubstituted β-ketoesters in high yields (91-99%) with high enantioselectivities (90-99% ee).
Synthesis of (2R,3S) 3-amino-4-mercapto-2-butanol, a threonine analogue for covalent inhibition of sortases
Jung, Michael E.,Clemens, Jeremy J.,Suree, Nuttee,Liew, Chu Kong,Pilpa, Rosemarie,Campbell, Dean O.,Clubb, Robert T.
, p. 5076 - 5079 (2007/10/03)
L-Threonine 2 was converted in seven steps into the protected aminomercaptoalcohol 8, a threonine mimic. This compound 8 was coupled to various oligopeptides to produce two different tetrapeptide analogues, for example, 11 and 17, which were shown to inhibit the Sortase enzymes (SrtA and SrtB) via covalent attachment of the thiol groups of 11 and 17 to the catalytically active cysteine residue of the Sortase enzymes.
New highly active taxoids from 9β-dihydrobaccatin-9,10-acetals. Part 4
Takeda, Yasuyuki,Uoto, Kouichi,Chiba, Jun,Horiuchi, Takao,Iwahana, Michio,Atsumi, Ryo,Ono, Chiho,Terasawa, Hirofumi,Soga, Tsunehiko
, p. 4431 - 4447 (2007/10/03)
It was shown that a new taxane analogue 3, which exhibited both in vitro antitumor activity and in vivo efficacy by both iv and po administration, was prone to be metabolized by human liver microsomes. We identified a major metabolite, M-1, generated by h
A strategy for the asymmetric aminohomologation of α,β-dihydroxy aldehydes: Application to the synthesis of the southwest tripeptide segment of echinocandin B
Palomo, Claudio,Oiarbide, Mikel,Landa, Aitor
, p. 41 - 46 (2007/10/03)
The synthesis of the (2S,3S,4S)-3,4-dihydroxyhomotyrosine amino acid segment, present in echinocandin B, in its activated form ready for peptide coupling is described. The key steps of the approach are the enantioselective AD reaction of 4-methoxycinnamic
