Klaus Albertshofer
Scripps Research Institute
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Publication
Featured researches published by Klaus Albertshofer.
Organic Letters | 2008
S. S. V. Ramasastry; Klaus Albertshofer; and Naoto Utsumi; Carlos F. Barbas
A novel organocatalyst was developed that effectively catalyzed the reactions of unprotected or protected dihydroxyacetone with a variety of aldehydes to provide syn-aldol products with good yields and ee values up to >99%. Significantly, this amide catalyst was effective with a variety of nonaromatic aldehyde acceptors that had proven difficult in the presence of other catalysts. Reactions of protected dihydroxyacetone proceeded in aqueous media without addition of organic solvents.
Organic Letters | 2012
Klaus Albertshofer; Bin Tan; Carlos F. Barbas
A novel organocatalytic strategy for the synthesis of highly substituted spirocyclopentaneoxindoles was developed employing simple nitrostyrenes and 3-substituted oxindoles as starting materials. Michael-Henry cascade reactions, enabled through cinchona alkaloid organocatalysis, provided products in high yield and excellent enantioselectivity in a single step.
Organic Letters | 2012
Klaus Albertshofer; Kimberly E. Anderson; Carlos F. Barbas
The assembly of complex spirocyclopentaneoxindoles via a novel organocatalytic iminium-enamine cascade process is reported. Reactions between 3-substituted oxindoles and α,β-unsaturated aldehydes catalyzed by second generation prolinol ethers provided the desired products in high yield with excellent levels of enantioselectivity in a single step.
Organic Letters | 2013
Klaus Albertshofer; Bin Tan; Carlos F. Barbas
An efficient organocatalytic asymmetric [3 + 2] cycloaddition reaction between 3-substituted methylenebenzofuranone derivatives and diverse Morita-Baylis-Hillman carbonates to provide complex polysubstituted spirocyclopentenebenzofuranone scaffolds in a single step is reported. C2-symmetric phospholanes were efficient nucleophilic catalysts of this transformation under mild conditions, providing reaction products comprised of three consecutive stereocenters, including one all-carbon center, with excellent enantioselectivity.
Journal of Medicinal Chemistry | 2010
Edward Wancewicz; Martin Maier; Andrew M. Siwkowski; Klaus Albertshofer; Theodore M. Winger; Andres Berdeja; Hans Gaus; Timothy A. Vickers; C. Frank Bennett; Brett P. Monia; Richard H. Griffey; Christopher J. Nulf; Jiaxin Hu; David R. Corey; Eric E. Swayze; Garth A. Kinberger
A peptide nucleic acid (PNA) targeting a splice junction of the murine PTEN primary transcript was covalently conjugated to various basic peptides. When systemically administered to healthy mice, the conjugates displayed sequence-specific alteration of PTEN mRNA splicing as well as inhibition of full length PTEN protein expression. Correlating activity with drug concentration in various tissues indicated strong tissue-dependence, with highest levels of activity observed in adipose tissue. While the presence of a peptide carrier was found to be crucial for efficient delivery to tissue, little difference was observed between the various peptides evaluated. A second PNA-conjugate targeting the murine insulin receptor primary transcript showed a similar activity profile, suggesting that short basic peptides can generally be used to effectively deliver peptide nucleic acids to adipose tissue.
Journal of the American Chemical Society | 2008
Haile Zhang; Susumu Mitsumori; Naoto Utsumi; Masanori Imai; † Noemi Garcia-Delgado; Maria Mifsud; Klaus Albertshofer; Paul Ha-Yeon Cheong; K. N. Houk; Fujie Tanaka, ,† and; Carlos F. Barbas
Angewandte Chemie | 2007
S. S. V. Ramasastry; Klaus Albertshofer; Naoto Utsumi; Fujie Tanaka; Carlos F. Barbas
Journal of Organic Chemistry | 2006
Jeff T. Suri; Susumu Mitsumori; Klaus Albertshofer; Fujie Tanaka; Carlos F. Barbas
Organic Letters | 2006
Naidu S. Chowdari; Moballigh Ahmad; Klaus Albertshofer; and Fujie Tanaka; Carlos F. Barbas
Journal of Medicinal Chemistry | 2005
Klaus Albertshofer; Andrew M. Siwkowski; Edward Wancewicz; Christine Esau; Tanya Watanabe; Kenji C. Nishihara; Garth A. Kinberger; Leila Malik; Anne B. Eldrup; Muthiah Manoharan; Richard S. Geary; Brett P. Monia; Eric E. Swayze; Richard H. Griffey; and C. Frank Bennett; Martin Maier