Morera Enrico, Pinnen Francesco, Lucente Gino
Dipartimento di Studi Farmaceutici and Centro di Studio per la Chimica del Farmaco del CNR, Università degli Studi di Roma "La Sapienza", P.le A. Moro 5, 00185 Roma, Italy.
Org Lett. 2002 Apr 4;4(7):1139-42. doi: 10.1021/ol0255458.
[reaction: see text]1,2-Dithiolanes present several points of interest for both peptide and medicinal chemistry, yet no chiral alpha-amino acids containing this five-membered heterocyclic system are available. We report here the first synthesis of N- and C-protected derivative of (S)-2-amino-3-(1,2-dithiolan-4-yl)propionic acid (Adp) and its 1,3-dithiolic form.
[反应：见正文]1,2-二硫杂环戊烷对肽化学和药物化学都有几个值得关注的点，但目前还没有含有这种五元杂环体系的手性α-氨基酸。我们在此报告(S)-2-氨基-3-(1,2-二硫杂环戊烷-4-基)丙酸（Adp）及其1,3-二硫醇形式的N-和C-保护衍生物的首次合成。
