Synthesis of a 10,000 member 1,5-benzodiazepine-2-one library by the directed sorting method.
The solid-phase synthesis of a 10,000 member combinatorial library of 1,5-benzodiazepine-2-one derivatives is reported. The 3-amino-1,5-benzodiazepine-2-one scaffold was prepared in solution, and the benzamide nitrogen was used as a point of attachment to the resin. The 5-aniline and 3-amine were then used as points of diversity. A 10,000 member library was synthesized using the Irori directed sorting system, and after analysis of a representative sample from the library, the Irori system was used to remove the compounds of lower purity.
Herpin
T F
TF
Rhône-Poulenc Rorer Research and Development, 500 Arcola Road, Collegeville, Pennsylvania 19426, USA.
Van Kirk
K G
KG
Salvino
J M
JM
Yu
S T
ST
Labaudinière
R F
RF
D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry; D000595:Amino Acid Sequence; D014151:Anti-Anxiety Agents / Q000737:chemistry*; D001570:Benzodiazepinones / Q000138:chemical synthesis* / Q000737:chemistry*; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D015195:Drug Design; D004399:Dynorphins / Q000737:chemistry; D008024:Ligands; D008969:Molecular Sequence Data; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000588:Amines; D014151:Anti-Anxiety Agents; D001570:Benzodiazepinones; D008024:Ligands; D004399:Dynorphins