Chemical library synthesis

Parlow JJ, Devraj RV, South MS (1999) Solution-phase chemical library synthesis using polymer-assisted purification techniques. Curr Opin Chem Biol 3 320-336... 

Drug Discovery Chemical library synthesis Purity and identity determination Yes Low... 

The recent development of parallel and combinatorial chemical library synthesis has created a renewed interest in polymeric solid-phase reagents. They offer the advantage of... 

In 1999, Salvino and coworkers developed a novel supported Weinreb amide resin tli3,t facilitates p3T3.11cl synthesis of aldehydes nd ketones on 3. sc3le useful for chemical library synthesis (Scheme 107). 

POLYMER-ASSISTED SOLUTION-PHASE METHODS FOR CHEMICAL LIBRARY SYNTHESIS... 

This chapter categorizes major approaches to polymer-assisted solution-phase syntheses. It highlights recent reports describing multistep chemical library synthesis using only polymer-assisted purifications, so disproving the assertion that solution-phase syntheses of libraries is limited only to... 

The first report of resin capture in solution-phase chemical library synthesis involved the covalent capture of solution-phase Ugi reaction products onto a functionalized polystyrene resin.73 Excess reactants, reagents, and reagent byproducts were washed away from the resin-captured intermediates. Further manipulation and release afforded purified solution-phase products for screening. More recently the same group reported on resin capture as a technique for the preparation of tetrasubstituted olefin libraries.74 75 As illustrated in Scheme 5, m-vinyl di-boryl esters were reacted with aryl halides (R3ArX) in parallel Suzuki reactions, leading to solution-phase intermediates. Another Suzuki reaction, this time with the... 

Flynn, D. L. Devraj, R. V. Parlow, J. J. Recent Advances in Polymer-Assisted Solution-Phase Chemical Library Synthesis and Purification, Curr. Opin. Drug Disc. Dev. 1998, 7, 41. 

There are many variations of combinatorial chemistry, and all have distinct advantages and disadvantages. A comprehensive description of the different techniques is beyond the scope of this chapter. In the following sections, a few examples will highlight the main features common to most combinatorial approaches to library synthesis. This section contains a considerable amount of synthetic chemistry. The goal of this section is not to teach organic synthesis but instead to demonstrate the basics of chemical library synthesis. Do not get lost in the synthesis Focus instead on the characteristics and qualities specific to each combinatorial technique. 

Salvino JM, Kumar NV, Orton E, Airey J, Kiesow T, Crawford K., Mathew R, KroUkowski P, Drew M, Engers D, Kro-likowski D, Herpin T, Gardyan M, McGeehan G, Labaudiniere R. Polymer-supported tetrafluorophenol a new activated resin for chemical library synthesis. J. Comb. Chem. 2000 2 691-697. Baxendale IR, Ley SV. Polymer-supported reagents for multi-step organic synthesis appUcation to the synthesis of sildenafil. Bioorg. Med. Chem. Lett. 2000 10 1983-1986. 

Linclau B, Sing AK, Curran DP. Organic-Fluorous phase switches a fluorous amine scavenger for purification in solution phase parallel synthesis. J Org Chem. 1999 64 2835-2842. Parlow JJ. Polymer-assisted solution-phase chemical library synthesis. Curr. Opin. Drug Discov. Devel. 2005 8 757-775. 

There are two ways to generate a collection of ligand molecules for immobilization on surfaces chemical library synthesis on micro- or macrobeads and diversity-oriented parallel synthesis of tethered unique compounds (Darvas et al., 2004). 

Flynn, D.L., Devraj, R.V., and Parlow, J.J., Recent advances in polymer-assisted solution-phase chemical library synthesis and purihcation, Curr. Opin. Drug Discovery Dev., 1, 41, 1998. 

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