𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Triphosgene as highly efficient reagent for the solid-phase coupling of N-alkylated amino acids—total synthesis of cyclosporin O

✍ Scribed by Bernd Thern; Joachim Rudolph; Günther Jung


Publisher
Elsevier Science
Year
2002
Tongue
French
Weight
217 KB
Volume
43
Category
Article
ISSN
0040-4039

No coin nor oath required. For personal study only.

✦ Synopsis


A novel, highly efficient and racemization free coupling procedure for sterically hindered N-alkyl amino acids has been developed using triphosgene and a combination of diisopropylethyl amine (DIEA) and collidine at room temperature. Its efficiency was demonstrated by comparison with other coupling methods for N-alkylated amino acids and by solid-phase synthesis of the immunosuppressant cyclosporin O which was obtained in excellent purity and yield.


📜 SIMILAR VOLUMES