%D 2018
%N 1
%J JOURNAL OF FLOW CHEMISTRY
%R 3374072
%O FELTÖLTŐ: Nonn Melinda nonn.melinda@pharm.u-szeged.hu
Funding Agency and Grant Number: Hungarian Research Foundation (OTKA) [K 115731];  [GINOP-2.3.2-15-2016-00014];  [UNKP-16-4-III]
            Funding text: We are grateful to the Hungarian Research Foundation (OTKA No. K 115731). The financial support of the GINOP-2.3.2-15-2016-00014 project is acknowledged. Supported by the UNKP-16-4-III New National Excellence Program of the Ministry of Human Capacities
%I szte
%X A rapid, simplified and highly efficient continuous-flow solid-phase peptide synthesis technology is reported for the direct synthesis of mono and multiple N-methylated cyclic alanine and valine peptides. Through an optimization study, we find that only 1.5 equivalents of the amino acids are sufficient for the couplings to maintain excellent conversions. Importantly, the technology is outstandingly sustainable, since three chemical steps are cancelled from the procedure and low amount of solvent is used, compared to traditional technologies. Furthermore, it is also applicable to the coupling of challenging amino acids, since pentavalines were constructed with high yield. The technology was successfully upscaled and peptide cyclization was carried out too.
%L publicatio14629
%T Sustainable synthesis of N-methylated peptides in a continuous-flow fixed bed reactor
%A  SzloszĂĄr Aliz
%A  MĂĄndity IstvĂĄn
%A  FĂźlĂśp Ferenc
%V 8
%P 21-27