Parallel Chemistry in the 21st Century

Alan Long1

1 SCYNEXIS, Research Triangle Park, North Carolina
Publication Name:  Current Protocols in Pharmacology
Unit Number:  Unit 9.16
DOI:  10.1002/0471141755.ph0916s58
Online Posting Date:  September, 2012
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Abstract

The tool chest of techniques, methodologies, and equipment for conducting parallel chemistry is larger than ever before. Improvements in the laboratory and developments in computational chemistry have enabled compound library design at the desks of medicinal chemists. This unit includes a brief background in combinatorial/parallel synthesis chemistry, along with a discussion of evolving technologies for both solid‐ and solution‐phase chemistry. In addition, there are discussions on designing compound libraries, acquisition/procurement of compounds and/or reagents, the chemistry and equipment used for chemical production, purification, sample handling, and data analysis. Curr. Protoc. Pharmacol. 58:9.16.1‐9.16.16. © 2012 by John Wiley & Sons, Inc.

Keywords: parallel chemistry; combinatorial chemistry; fluorous chemistry; multi‐component reactions; library design; laboratory equipment; DOS; diversity oriented synthesis

     
 
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Table of Contents

  • Brief History
  • Evolving Chemistries
  • New Directions
  • The Process
  • Conclusion
  • Literature Cited
  • Figures
     
 
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Materials

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Figures

Videos

Literature Cited

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   Curran, D.P., Moura‐Letts, G., and Pohlman, M. 2006a. Solution‐phase mixture synthesis with fluorous tagging en route: Total synthesis of an eight‐member stereoisomer library of Passifloricins. Angew. Chem. Int. Ed. 45:2423‐2426.
   Curran, D.P., Zhang, Q., Richard, C., Lu, H., Gudipati, V., and Wilcox, C.S. 2006b. Total synthesis of a 28‐member stereoisomer library of Murisolins. J. Amer. Chem. Soc. 128:9561‐9573.
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   Hughes, P.F., Graham, T.H., and Mendoza, J.S. 2004. Array reactors for parallel synthesis. J. Comb. Chem. 6:308‐311.
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Internet Resources
   http://www.sigmaaldrich.com/etc/medialib/docs/Aldrich/Brochure/al_chemfile_v5_n11.Par.0001.File.tmp/al_chemfile_v5_n11.pdf
  A listing of polymer‐supported reagents with synthetic examples.
   http://www.innovasyn.com/index.php?content=drewpage
  A very informative resource for the reader: Drew University Residential Medicinal Chemistry lecture on Chemical Diversity given by Philip Hughes in 2005. Products for parallel chemistry requiring specialized conditions are also described.
   http://www‐oc.chemie.uni‐regensburg.de/OCP/ch/chv/oc22/script/CombiChem‐Handout‐part2.pdf
  An excellent slide deck covering many facets of combinatorial chemistry.
   http://us.chemdiv.com/
  A Web site providing chemical libraries for sale and other services related to medicinal chemistry.
   http://www.lifechemicals.com/
  A Web site providing chemical libraries for sale and other services related to medicinal chemistry.
   http://www.chembridge.com/
  A Web site providing chemical libraries for sale and other services related to medicinal chemistry.
   http://www.asinex.com/
  A Web site providing chemical libraries for sale.
  www.emolecules.com
  A Web site providing free online searching for chemical compounds.
  https://scifinder.cas.org/
  A Web site providing fee‐based searching capabilities for chemical compounds and much more.
   http://www.radleys.com/
  A Web site with parallel synthesizers for round‐bottomed flasks and vials. Also offered are systems for solvent evaporation.
   http://us.mt.com/us/en/home.html
  A Web site with both the Bohdan and Mettler‐Toledo brands of automated weighing (and other) laboratory equipment.
   http://www.zinsserna.com/products_chemistry.htm
  A Web site showing equipment for automated parallel chemistry.
   http://www.buchi.com/Home.1.0.html
  A Web site with equipment for parallel synthesis and evaporation.
   http://www.heidolph‐instruments.com/
  A Web site with equipment for parallel synthesis and other laboratory equipment.
   http://www.tecan.com/
  A Web site offering robotic systems for liquid handling in parallel chemistry.
   http://www.chemspeed.com/
  A Web site offering robotic systems for liquid handling in parallel chemistry.
   http://www.gilson.com/en/
  A Web site offering robotic systems for liquid handling in parallel chemistry or purifications.
   http://www.biodot.com/
  A Web site with equipment for the automated weighing of dry samples.
   http://www.innovateengineering.com/
  A Web site with equipment for the automated weighing of dry samples.
   http://www.cem.com/
  A Web site with equipment for conducting microwave chemistry.
   http://www.biotage.com/
  A Web site with equipment for microwave chemistry, parallel purifications, and solvent evaporation.
   http://www.anton‐paar.com/
  A Web site offering products for microwave chemistry.
   http://www.isco.com/
  A Web site with equipment for performing parallel purifications.
   http://www.genevac.com/
  A Web site offering products for centrifugal evaporation.
   http://www.mimotopes.com/
  A Web site offering the SynPhase Lanterns for solid‐phase synthesis.
   http://www/scynexis.com
  A Web site for a contract research organization providing Discovery Research, Integrated Parasitology, and Integrated Pharmaceutical solutions for a variety of global clients.
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