非表示:
キーワード:
PEPTIDYL-PROLYL ISOMERASE; IMMUNOSUPPRESSANT FK506; ASYMMETRIC
EPOXIDATION; DERIVATIVES; LIGANDS; FKBP52; INHIBITION; EFFICIENCY;
RAPAMYCIN; KETONE
要旨:
A stereoselective synthesis of a derivatized bicyclic [4.3.1]decane scaffold based on an acyclic precursor is described. The key steps involve a Pd-catalyzed sp(3)sp(2) Negishi-coupling, an asymmetric Shi epoxidation, and an intramolecular epoxide opening. Representative derivatives of this novel scaffold were synthesized and found to be potent inhibitors of the psychiatric risk factor FKBP51, which bound to FKBP51 with the intended molecular binding mode.
