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Trident Library Synthesizer For Automation of Multistep Solution Phase Synthesis

Presented by

Jeff Labadie,

Argonaut Technologies, 887 Industrial Road, Suite G, San Carlos, CA 94070.

At the 4/27/2000 San Diego LRIG Vendor Show and Presentations.

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Table of Contents

Trident Library Synthesizer For Automation of Multistep Solution Phase Synthesis

Agenda

Historical Perspective

Goals of Lead Optimization

Applications for Automated Synthesis are Changing

Range of Chemistries

High Throughput Lead Optimization Workflow

Solution Phase Synthesis:

Critical Parameters

Solution Phase Library Synthesis:

Purification Methods

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Synthesize Without Compromise

The Heart of the System

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Reagent & Solvent Delivery

Validation of System Using

Precise Air-Sensitive Deliveries

Validation of System: Results

High Throughput Lead Optimization Workflow

Trident Modules:

Scalable Technology

Chemistry Development

and Rehearsal

Purification

Where Trident Fits into the Process

Chemistry Validation

Parallel Purification Methods:

Working with "Hot" Reagents

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Working with Precipitates

2-Aminothiazoles

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Split Synthesis on Trident

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Split Synthesis

Automating Tedious Purification Steps

Trident SPS:

Liquid-Liquid Extraction



Liquid-Liquid Extraction Protocols



Multistep Synthesis

Benzimidazoles

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Focused Library Synthesis of 48 Benzimidazoles on Automated Platform

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Trident Synthesizer:

Air-sensitive reagents

Automated Approach

Semi-Automated Approach

Trident Technology provides a Flexible Synthesis platform



Acknowledgement

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