Abstract
Equation presented A practical, chromotography-free asymmetric synthesis was developed for the large scale preparation of an endothelin receptor antagonist 2. This synthesis includes a new efficient process for the preparation of 6-bromo-2,3-dihydrobenzofuran, a stereoselective conjugate addition of an aryllithium followed by stereospecific addition of the Grignard reagent of the top aryl bromide, and an aminophosphate-mediated sterospecific intramolecular enolate alkylation, which led to the formation of the five-membered ring bearing three contiguous asymmetric centers.
Original language | English (US) |
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Pages (from-to) | 3357-3360 |
Number of pages | 4 |
Journal | Organic letters |
Volume | 3 |
Issue number | 21 |
DOIs | |
State | Published - Oct 18 2001 |
Externally published | Yes |
All Science Journal Classification (ASJC) codes
- Biochemistry
- Physical and Theoretical Chemistry
- Organic Chemistry