Abstract
A highly efficient method for the synthesis of medium-sized lactams based on intramolecular Staudinger-aza-Wittig reaction of ω-azido pentafluorophenyl ester has been developed. A variety of 7-10 membered lactams were synthesized in excellent yields. Application of the method to the synthesis of analogues of a potent γ-secretase inhibitor LY411575 and their biological evaluation are also described.
Original language | English |
---|---|
Pages (from-to) | 2323-2326 |
Number of pages | 4 |
Journal | Tetrahedron Letters |
Volume | 45 |
Issue number | 11 |
DOIs | |
Publication status | Published - 2004 Feb 8 |
Externally published | Yes |
Keywords
- Aza-Wittig reaction
- Medium-sized lactams
- Staudinger reaction
- Structure-activity relationship
- γ-Secretase inhibitor
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry