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Build/couple/pair strategy for the synthesis of stereochemically diverse macrolactams via head-to-tail cyclization.

Abstract：

:A build/couple/pair (B/C/P) strategy was employed to generate a library of 7936 stereochemically diverse 12-membered macrolactams. All 8 stereoisomers of a common linear amine precursor were elaborated to form the corresponding 8 stereoisomers of two regioisomeric macrocyclic scaffolds via head-to-tail cyclization. Subsequently, these 16 scaffolds were further diversified via capping of two amine functionalities on SynPhase Lanterns. Reagents used for solid-phase diversification were selected using a sparse matrix design strategy with the aim of maximizing coverage of chemical space while adhering to a preset range of physicochemical properties.

journal_name

ACS Comb Sci

journal_title

ACS combinatorial science

authors

Fitzgerald ME,Mulrooney CA,Duvall JR,Wei J,Suh BC,Akella LB,Vrcic A,Marcaurelle LA

doi

10.1021/co200161z

subject

Has Abstract

pub_date

2012-02-13 00:00:00

pages

89-96

issue

2

eissn

2156-8952

issn

2156-8944

journal_volume

14

pub_type

杂志文章

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