Automated Parallel, Multi-Step Polymer-Assisted Solution Phase (PASP) Synthesis of Substituted Benzimidazole Derivatives

Author(s): Stephen P. Andrews, Daniel Jonsson, Brian H. Warrington, Mark Ladlow

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 7 , Issue 2 , 2004


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Abstract:

The automated polymer-assisted solution phase (PASP) synthesis of a 72 member library of 2- alkylthio-benzimidazoles 16 and benzimidazolin-2-ones 17 using commercially available robotic workstations is described. By incorporating both automated aqueous work-ups, in-line scavenging and catch and release protocols the desired compounds were obtained directly in good yields and excellent purities without the need for conventional chromatographic purification. The synthesis described demonstrates how both manual and automated equipment may be utilised together to provide a versatile approach that facilitates parallel compound synthesis.

Keywords: polymer-assisted, solution phase, benzimidazole, capture and release

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Article Details

VOLUME: 7
ISSUE: 2
Year: 2004
Page: [163 - 178]
Pages: 16
DOI: 10.2174/138620704773120847
Price: $65

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