Synthesis of a first thiophene containing analog of the HIV protease inhibitor nelfinavir

• Published in: Tetrahedron letters Vol. 45; no. 13; pp. 2797 - 2799
• Main Authors: Bonini, Carlo, Chiummiento, Lucia, De Bonis, Margherita, Funicello, Maria, Lupattelli, Paolo
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 22-03-2004
• Subjects: HIV-Pr inhibitors; Hydroxyethylamine (HEA) inhibitors; Nelfinavir analog; Peptidomimetics; Sulfite; Thiophene; Sulfite; HIV-Pr inhibitors; Hydroxyethylamine (HEA) inhibitors; Thiophene; Peptidomimetics; Nelfinavir analog
• ISSN: 0040-4039; 1873-3581
• DOI: 10.1016/j.tetlet.2004.02.026

A stereoselective and efficient preparation of a thiophene containing intermediate
2
from ethyl 3-thienyl propenoate
4
as the core of new possible HIV protease inhibitors is described.
A stereoselective and efficient preparation of a thiophene containing intermediate
2
from ethyl 3-thienyl propenoate
4
as the core of new possible HIV protease inhibitors is described. The chiral intermediate has been successfully used for the preparation of the analog
1
of the potent HIV inhibitor nelfinavir.