TY - JOUR
T1 - Synthesis of 1,4,5 trisubstituted γ-lactams via a 3-component cascade reaction
AU - Petersen, Michael Åxman
AU - Mortensen, Michael Agerup
AU - Cohrt, A. Emil
AU - Petersen, Rico
AU - Wu, Peng
AU - Fleury-Brégeot, Nicolas
AU - Morgentin, Rémy
AU - Lardy, Claude
AU - Nielsen, Thomas Eiland
AU - Clausen, Mads Hartvig
PY - 2015
Y1 - 2015
N2 - A three component one-pot cascade reaction was developed for the synthesis of 1,4,5-trisubstituted γ-lactams. The resulting scaffold can be modified independently at three positions, two of which are conveniently accessed by changing the components of the one-pot reaction. The phases of building block generation, scaffold synthesis and subsequent appendage modification were adapted to library production, which resulted in a screening library of 500 compounds.
AB - A three component one-pot cascade reaction was developed for the synthesis of 1,4,5-trisubstituted γ-lactams. The resulting scaffold can be modified independently at three positions, two of which are conveniently accessed by changing the components of the one-pot reaction. The phases of building block generation, scaffold synthesis and subsequent appendage modification were adapted to library production, which resulted in a screening library of 500 compounds.
KW - γ-Lactams
KW - Cascade reaction
KW - One-pot reaction
KW - Molecular diversity
KW - Library production
U2 - 10.1016/j.bmc.2015.01.041
DO - 10.1016/j.bmc.2015.01.041
M3 - Journal article
C2 - 25684425
SN - 0968-0896
VL - 23
SP - 2695
EP - 2698
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
IS - 11
ER -