Demonstration on Pilot-Plant Scale of the Utility of 1,5,7-Triazabicyclo[4.4.0]dec-5-ene (TBD) as a Catalyst in the Efficient Amidation of an Unactivated Methyl Ester

2012/11/10 by Franz J. Weiberth, Yong Yu, Witold Subotkowski +1 · 1 voice
Biochemistry, Genetics and Molecular Biology · Chemistry · #Asymmetric Hydrogenation and Catalysis #Chemical Synthesis and Analysis #Chemical Synthesis and Reactions

paper · doi:10.1021/op300210j

openalex publication_date 2012/11/10 · openalex created_date 2025/10/10 · openalex updated_date 2026/06/16

Abstract

The utility of 1,5,7-triazabicyclo[4.4.0]dec-5-ene as a reagent to facilitate efficient amide formation by reaction of an amine with an unactivated ester was demonstrated on pilot-plant scale as a key step in the synthesis of an H-PGDS inhibitor.

Discussions

• Alternatively, another personal fav, have you looked at TBD-mediated ester functionalization? e.g. doi.org/10.1021/op30... [bsky, 2 points, 2 comments]

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