Ontology highlight
ABSTRACT:
SUBMITTER: Han J
PROVIDER: S-EPMC6943542 | biostudies-literature | 2019 Dec
REPOSITORIES: biostudies-literature
Molecules (Basel, Switzerland) 20191210 24
Enantiomerically pure derivatives of 2-amino-4,4,4-trifluorobutanoic acid are in great demand as bioisostere of leucine moiety in the drug design. Here, we disclose a method specifically developed for large-scale (>150 g) preparation of the target (<i>S</i>)-<i>N</i>-Fmoc-2-amino-4,4,4-trifluorobutanoic acid. The method employs a recyclable chiral auxiliary to form the corresponding Ni(II) complex with glycine Schiff base, which is alkylated with CF<sub>3</sub>-CH<sub>2</sub>-I under basic condi ...[more]