Combinatorial solid-phase synthesis of hapalosin mimetics
Research output: Contribution to journal › Journal article › Research › peer-review
The solid-phase synthesis of a small library of mimetics of the cyclic depsipeptide hapalosin is described. 3-Amino-4-hydroxy-5-nitrobenzoic acid was anchored through the anilino moiety to a backbone amide linker (BAL) handle support. Using chemoselective reactions and without the need for protecting group manipulations, the benzoic acid group was first amidated, then the aniline nitrogen was acylated, and finally the nitro group was reduced to an amine and acylated or reductively alkylated, to generate a 12-member library.
|Journal||Journal of Combinatorial Chemistry|
|Number of pages||8|
|Publication status||Published - 1 Mar 2000|