✦ LIBER ✦
A short synthesis of the HIV-protease inhibitor nelfinavir via a diastereoselective addition of ammonia to the α,β-unsaturated sulfoxide derived from (R)-glyceraldehyde acetonide
✍ Scribed by Dawei Ma; Bin Zou; Wei Zhu; Huadong Xu
- Publisher
- Elsevier Science
- Year
- 2002
- Tongue
- French
- Weight
- 216 KB
- Volume
- 43
- Category
- Article
- ISSN
- 0040-4039
No coin nor oath required. For personal study only.
✦ Synopsis
Diastereoselective Michael addition of ammonia to sulfoxide 3a derived from (R)-glyceraldehyde acetonide provides amine 4a, which is converted into Nelfinavir using BF 3 •Et 2 O/NaI reduction and subsequent coupling reactions as key steps.