Combinatorial Chemistry in Pharmaceutical Chemistry
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Questions and Answers

In combinatorial chemistry, why has there been much interest in using solution-phase chemistry for the preparation of combinatorial libraries?

  • To avoid mixtures of products that occur in one-bead synthesis
  • To reduce the time and resources required to develop and optimize reaction conditions for solid support reactions (correct)
  • To increase the yield of reactions that cannot be run on solid supports
  • To ensure that all reactions occur between amines and acid chlorides

    • What is the advantage of one-bead synthesis over solution-phase combinatorial chemistry?

  • One-bead synthesis results in one-compound synthesis (correct)
  • One-bead synthesis results in a mixture of products
  • One-bead synthesis allows for reactions between amines and chlorides only
  • One-bead synthesis is more time-consuming than solution-phase combinatorial chemistry

    • Why are many reactions unable to be run on solid supports in combinatorial chemistry?

  • Due to the lack of interest in solid support reactions
  • Because it takes time and resources to develop and optimize reaction conditions for solid support reactions
  • Because solid support reactions result in poor yields (correct)
  • Because solid support reactions lead to a mixture of products

    • What is the outcome of reacting a set of 10 amines with 10 acid chlorides in one flask, using the chosen reactants and conditions?

    <p>A mixture of 100 amides, one for each possible combination of amine and acid chloride</p> Signup and view all the answers

    Why does solution-phase combinatorial chemistry often lead to a mixture of products?

    <p>Because it involves reacting multiple components in one flask</p> Signup and view all the answers

    What is the major limitation of running reactions on solid supports in combinatorial chemistry?

    <p>Poor yields or failed reactions</p> Signup and view all the answers

    What is the main difference between solid-phase chemistry and solution-phase chemistry?

    <p>The use of soluble polymers as support in solution-phase chemistry.</p> Signup and view all the answers

    Which type of soluble polymer can be liquid or solid at room temperature, depending on the degree of polymerization?

    <p>PEG</p> Signup and view all the answers

    What is the main function of terminal amino groups in dendrimers?

    <p>To act as a support for the product.</p> Signup and view all the answers

    What is the composition of fluorous phases used as a soluble support for synthesis?

    <p>Long chains of (-𝐶𝐹2-) groups attached to a silicon atom.</p> Signup and view all the answers

    How do researchers at Harvard use complementary DNA in synthesis?

    <p>To encourage molecules to react by attaching short strands of DNA or RNA.</p> Signup and view all the answers

    What is the purpose of recursive deconvolution in identifying the active component in a mixture?

    <p>To narrow down the active component to one of three possible structures.</p> Signup and view all the answers

    What is the purpose of tagging in combinatorial synthesis?

    <p>To identify the structure present on a bead.</p> Signup and view all the answers

    What is the main challenge associated with purification in mixture-based experiments?

    <p>Difficulty of removing unwanted material and the necessity for purification at each step.</p> Signup and view all the answers

    What are the yields of products often found to be in mixture-based experiments?

    <p>~90% or better</p> Signup and view all the answers

    What can be tested to eventually find the structure(s) responsible for activity?

    <p>Smaller subsets of amines and chlorides</p> Signup and view all the answers

    In combinatorial chemistry, what is the main challenge associated with using solution-phase chemistry for the preparation of combinatorial libraries?

    <p>Formation of mixtures of products leading to purification challenges</p> Signup and view all the answers

    What is the major limitation of running reactions on solid supports in combinatorial chemistry?

    <p>Poor yields or failed reactions</p> Signup and view all the answers

    What is the purpose of recursive deconvolution in identifying the active component in a mixture?

    <p>To separate and identify the individual components in a mixture</p> Signup and view all the answers

    Why are many reactions unable to be run on solid supports in combinatorial chemistry?

    <p>Formation of mixtures of products</p> Signup and view all the answers

    What can be tested to eventually find the structure(s) responsible for activity in combinatorial chemistry?

    <p>The resulting mixture for activity</p> Signup and view all the answers

    What is the main difference between solid-phase chemistry and solution-phase chemistry in combinatorial chemistry?

    <p>Solution-phase chemistry results in one-compound synthesis</p> Signup and view all the answers

    What is the primary purpose of using soluble polymers as a support in solution-phase chemistry?

    <p>To readily separate the resulting product from any organic solvents and reaction by-products</p> Signup and view all the answers

    What is the main function of terminal amino groups in dendrimers?

    <p>To be used like the OH groups of PEG for the attachment of products</p> Signup and view all the answers

    What is the composition of fluorous phases used as a soluble support for synthesis?

    <p>Liquid Teflon consisting mainly of long chains of (-𝐶𝐹2-) groups attached to a silicon atom</p> Signup and view all the answers

    What is the main challenge associated with purification in mixture-based experiments?

    <p>Difficulty of removing unwanted material</p> Signup and view all the answers

    What is the primary purpose of recursive deconvolution in identifying the active component in a mixture?

    <p>Quicker than separately synthesizing all possible components</p> Signup and view all the answers

    What is the advantage of one-bead synthesis over solution-phase combinatorial chemistry?

    <p>Method of identifying the structure present on a bead</p> Signup and view all the answers

    Why has there been much interest in using solution-phase chemistry for the preparation of combinatorial libraries?

    <p>Solution-phase chemistry often leads to a mixture of products</p> Signup and view all the answers

    What can be tested to eventually find the structure(s) responsible for activity?

    <p>Smaller subsets of amines and chlorides</p> Signup and view all the answers

    How do Harvard researchers use complementary DNA in synthesis?

    <p>By attaching short strands of complementary DNA or RNA to the structures to promote reaction</p> Signup and view all the answers

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