Aminomutase-Inspired Green Radical Amination
Jeffrey Lipshultz, Stony Brook University, $40,000 “Aminomutase-Inspired Green Radical Amination”
Author: Christiana Briddell
Overcoming light penetration challenges in photochemical reactions through a micro-LED packed bed reactor
Andrew Teixeira and Patricia Musacchio of Worcester Polytechnic Institute, $80,000 “Overcoming light penetration challenges in photochemical reactions through a micro-LED packed bed reactor”
Realizing the advantages of alternating polarity electrosynthesis at constant potential through controlled mass transport
Marcel Schreier and Shannon Stahl of the University of Wisconsin Madison, $80,000 “Realizing the advantages of alternating polarity electrosynthesis at constant potential through controlled mass transport”
Biocatalytic Synthesis of Phosphorothioate-Containing Nucleosides
Hans Renata of Rice University, $80,000 “Biocatalytic Synthesis of Phosphorothioate-Containing Nucleosides”
New technology for continuous flow liquid-phase sustainable synthesis of therapeutic peptides
Walter Cabri, Alessandra Tolomelli, and Lucia Ferrazzano, University of Bologna, $80,000 “New technology for continuous flow liquid-phase sustainable synthesis of therapeutic peptides”
Stereo-Controlled Liquid Phase Synthesis of Phosphorothioate Oligonucleotides on a Soluble Support
5′-O-(2-Methoxyisopropyl) (MIP)-protected 2′-deoxynucleosides as chiral P(V)-building blocks, based on the limonene-derived oxathiaphospholane sulfide, were synthesized and used for the assembly of di-, tri-, and tetranucleotide phosphorothioates on a tetrapodal pentaerythritol-derived soluble support. The synthesis cycle consisted of two reactions and two precipitations: (1) the coupling under basic conditions, followed by neutralization and precipitation and (2) an acid catalyzed 5′-O-deacetalization, followed by neutralization and precipitation. The simple P(V) chemistry together with the facile 5′-O-MIP deprotection proved efficient in the liquid phase oligonucleotide synthesis (LPOS). Ammonolysis released nearly homogeneous Rp or Sp phosphorothioate diastereomers in ca. 80% yield/synthesis cycle.