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As outlined in Scheme 1, the target molecules were synthesized by starting with the preparation of our key materials (1 4) according to the literature [13 15].
The synthesis of compounds D1 30 and F1 16 followed the general pathway as outlined in Scheme 1, gave satisfactory analytical and spectroscopic data, which were in full accordance with their depicted structures.
First, precursors 3 and 4 were prepared stepwise by solution phase peptide synthesis as outlined in Scheme 1 by use of propylphosphonic anhydride (T3P).
As outlined in Scheme 5, dihydroxylation of the terminal double bond with OsO4 and periodate cleavage of the resulting diol allowed the isolation of highly unstable aldehyde 21.
Therefore, to achieve labeling permutations that include C-3 and/or C-4, another strategy was developed as outlined in Scheme 1B.
Analogues 3 and 12 were synthesised as outlined in Scheme 2. Compounds 3 and 12 were designed to investigate additional positions at which a benzamidine or melamine moiety could be introduced into the quinol pharmacophore.
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Inhibitors were synthesized as outlined in schemes 1– 3; for a full description, see the Supplementary Online Data at http://www.biochemj.org/bj/457/bj4570497add.htm.htm
Seven new disaccharide dye conjugates were synthesized for this purpose, as outlined in Schemes 3 and S5 S8.
The synthesis of the new pyridinium bis amide)- strapped porphyrin macrocyclic fragment of the target [2]catenane was carried out as outlined in Schemes 1 and 2. Initially the bis amino porphyrin precursor Zn⋅ 3 a was prepared (Scheme 1).
Mnv agents EUKL-DOTA 3, cRGDfK-DOTA 5, and cRGDfK-IRDye800 6 were synthesized as outlined in Schemes 1 and 2. They represent the controls to which the in vitro binding affinities of the labeled HtBv agents could be compared.
After formation of a dodecin monolayer as outlined in Scheme 1 (1 3) we changed to an argon-saturated buffer and applied a negative potential (up to −650 mV vs. Ag/AgCl) but no release of tE was observed.
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