794525-86-3Relevant articles and documents
Stereoselective synthesis of photoreactive peptidomimetic γ-secretase inhibitors
Chun, Jiong,Yin, Ye Ingrid,Yang, Guangli,Tarassishin, Leonid,Li, Yue-Ming
, p. 7344 - 7347 (2007/10/03)
The first asymmetric synthesis of novel, potent photoreactive γ-secretase inhibitors 2 and 3 has been accomplished. Two Stereoselective methods for the preparation of lactone 9 are described. Protected benzophenone intermediate 19 is prepared via an aldol-elimination reaction followed by a PtO2-catalyzed asymmetric hydrogenation. Two routes leading from 19 to compounds 2 and 3 are evaluated. The application of 3 as an activity-based probe has been demonstrated by localizing γ-secretase activity in the plasma membrane of intact cells.