Applications of fluorine-containing amino acids for drug design

H Mei, J Han, KD Klika, K Izawa, T Sato… - European journal of …, 2020 - Elsevier
Fluorine-containing amino acids are becoming increasingly prominent in new drugs due to
two general trends in the modern pharmaceutical industry. Firstly, the growing acceptance of …

Tailor‐made amino acids and fluorinated motifs as prominent traits in modern pharmaceuticals

H Mei, J Han, S White, DJ Graham… - … A European Journal, 2020 - Wiley Online Library
Structural analysis of modern pharmaceutical practices allows for the identification of two
rapidly growing trends: the introduction of tailor‐made amino acids and the exploitation of …

Expedited synthesis of α-amino acids by single-step enantioselective α-amination of carboxylic acids

CX Ye, DR Dansby, S Chen, E Meggers - Nature Synthesis, 2023 - nature.com
The conversion of C‒H bonds to C‒N bonds offers a sustainable and economical strategy
for the synthesis of nitrogen-containing compounds. However, challenges regarding the …

Modular α-tertiary amino ester synthesis through cobalt-catalysed asymmetric aza-Barbier reaction

X Wu, H Xia, C Gao, B Luan, L Wu, C Zhang, D Yang… - Nature Chemistry, 2024 - nature.com
Unnatural chiral α-tertiary amino acids containing two different carbon-based substituents at
the α-carbon centre are widespread in biologically active molecules. This sterically rigid …

Stereoselective and site-specific allylic alkylation of amino acids and small peptides via a Pd/Cu dual catalysis

X Huo, R He, J Fu, J Zhang, G Yang… - Journal of the American …, 2017 - ACS Publications
We report a stereoselective and site-specific allylic alkylation of Schiff base activated amino
acids and small peptides via a Pd/Cu dual catalysis. A range of noncoded α, α-dialkyl α …

Catalyst‐Controlled Regiodivergent and Enantioselective Formal Hydroamination of N,N‐Disubstituted Acrylamides to α‐Tertiary‐α‐Aminolactam and β‐Aminoamide …

S Wang, L Shi, XY Chen, W Shu - … Chemie International Edition, 2023 - Wiley Online Library
Enantioenriched α‐tertiary‐α‐aminoacid and α‐chiral‐β‐aminoacid derivatives play an
important role in biological science and pharmaceutical chemistry. Thus, the development of …

Direct Asymmetric α-Alkylation of NH2-Unprotected Amino Acid Esters Enabled by Biomimetic Chiral Pyridoxals

P Ji, J Li, Y Tao, M Li, W Ling, J Chen, B Zhao - ACS Catalysis, 2023 - ACS Publications
Biosynthesis utilizes kinetic strategies to regulate the chemoselectivity for the
transformations of molecules containing multiple active reaction sites. But it is a grand …

Direct Asymmetric Synthesis of β-Bis-Aryl-α-Amino Acid Esters via Enantioselective Copper-Catalyzed Addition of p-Quinone Methides

FS He, JH Jin, ZT Yang, X Yu, JS Fossey… - ACS Catalysis, 2016 - ACS Publications
A highly efficient synthetic approach to unnatural chiral β-Ar, Ar′-α-amino acid esters
bearing two contiguous stereogenic centers has been developed. The first enantioselective …

Synthesis of Unnatural α-Amino Acid Derivatives via Photoredox Activation of Inert C(sp3)–H Bonds

F Babawale, K Murugesan, R Narobe, B König - Organic Letters, 2022 - ACS Publications
The synthesis of unnatural, tertiary amino acids is a challenging task. While decarboxylation–
radical addition has been an important strategy for their formation, the use of alkyl radicals …

Cyclic tailor-made amino acids in the design of modern pharmaceuticals

J Liu, J Han, K Izawa, T Sato, S White… - European Journal of …, 2020 - Elsevier
Tailor-made AAs are indispensable components of modern medicinal chemistry and are
becoming increasingly prominent in new drugs. In fact, about 30% of small-molecule …