Application of epimerisation-free amide coupling conditions to the synthesis of matrix metalloprotease inhibitor intermediates. Tetrahedron 1998;54:13825-32.Fray, et al, " Application of Epimerisation-Free Amide Coupling Conditions to the Synthesis of Matrix Metalloprotease Inhibitor Intermediates ", ...
Application of epimerisation-free amide coupling conditions to the synthesis of matrix metalloprotease inhibitor intermediates. Tetrahedron 1998;54:13825-32.Fray, et al, " Application of Epimerisation-Free Amide Coupling Conditions to the Synthesis of Matrix Metalloprotease Inhibitor Intermediates ", ...
Amide coupling using EDC/NHS «on:September 24, 2011, 08:09:59 PM » Due to some practical lab issues, I have to change the solvent conditions for a reaction between a PEG-amine and an amino acid NHS ester that I do a lot. Currently I run it in 10 mM PBS, pH 7.2 - I am...
The MMT-protected 5′-amino phosphoramidite monomer (either LNA1047or commercially available deoxythymidyl11) was dissolved in anhydrous MeCN to a concentration of 0.1 M immediately prior to use. The same coupling conditions as above were used, but the coupling time was extended to 10 min...
We began by screening various Cu-catalysts for the coupling of benzamide (2) with iodobenzene (3) under benign aqueous conditions (Supplementary Table 1). Most of the chemocatalysts tested typically operate at molar concentrations or under neat reaction conditions and were thus ineffective at the ...
The aromatic amine is a relatively poor nucleophile and thus coupling requires activation of monomers as acid chlorides and microwave assistance in order to be both rapid and essentially quantitative. Over the last number of years we have reported the SPS of increasingly elaborate oligomers, from ...
Goldberg Coupling Reaction Reaction of amide compounds with aromatic halides to yield multiply substituted amides. Buchwald-Hartwig Reaction Reaction of amide compounds with aromatic halides to yield multiply substituted amides. Copper-Catalyzed Reaction of Triaryl Bismuth and Amides ...
We disclose herein an amidation protocol which allows the use of low-molecular acetylene and its more activated homologue ethoxyacetylene as a sustainable alternative for state-of-the-art coupling agents. These procedures are convincing in terms of the amount, toxicity and separation of the formed ...
(CDI) followed by the addition of excess methylamine in THF provides the N-methyl amide prodrugs in moderate-to-good yields. The advantage of this method relates to the mild conditions for amide coupling of these rather expensive parent drug starting materials, which typically generates product ...
This allows the preparation of a bromide derivative that can be cross coupled under Suzuki coupling conditions, for instance using tri(tert-butyl)phosphine and Pd2(dba)3 as catalysts in the presence of a base, such as sodium carbonate. Conversion to the desired piperidine moiety is then ...