Combinatorial solid-phase synthesis of hapalosin mimetics
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Combinatorial solid-phase synthesis of hapalosin mimetics. / Olsen, Jacob A.; Jensen, Knud J.; Nielsen, John.
In: Journal of Combinatorial Chemistry, Vol. 2, No. 2, 01.03.2000, p. 143-150.Research output: Contribution to journal › Journal article › peer-review
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TY - JOUR
T1 - Combinatorial solid-phase synthesis of hapalosin mimetics
AU - Olsen, Jacob A.
AU - Jensen, Knud J.
AU - Nielsen, John
PY - 2000/3/1
Y1 - 2000/3/1
N2 - 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.
AB - 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.
M3 - Journal article
AN - SCOPUS:0034150453
VL - 2
SP - 143
EP - 150
JO - ACS Combinatorial Science
JF - ACS Combinatorial Science
SN - 2156-8952
IS - 2
ER -
ID: 131118506