Combinatorial Chemistry in Pharmaceutical Chemistry

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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?

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

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

Because it involves reacting multiple components in one flask Signup and view all the answers

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

Poor yields or failed reactions Signup and view all the answers

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

The use of soluble polymers as support in solution-phase chemistry. 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?

PEG Signup and view all the answers

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

To act as a support for the product. Signup and view all the answers

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

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

How do researchers at Harvard use complementary DNA in synthesis?

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

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

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

What is the purpose of tagging in combinatorial synthesis?

To identify the structure present on a bead. Signup and view all the answers

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

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

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

~90% or better Signup and view all the answers

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

Smaller subsets of amines and chlorides 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?

Formation of mixtures of products leading to purification challenges Signup and view all the answers

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

Poor yields or failed reactions Signup and view all the answers

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

To separate and identify the individual components in a mixture Signup and view all the answers

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

Formation of mixtures of products Signup and view all the answers

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

The resulting mixture for activity Signup and view all the answers

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

Solution-phase chemistry results in one-compound synthesis Signup and view all the answers

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

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

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

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

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

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

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

Difficulty of removing unwanted material Signup and view all the answers

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

Quicker than separately synthesizing all possible components Signup and view all the answers

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

Method of identifying the structure present on a bead Signup and view all the answers

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

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

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

Smaller subsets of amines and chlorides Signup and view all the answers

How do Harvard researchers use complementary DNA in synthesis?

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

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?

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

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

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

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

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

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

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

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

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

How do researchers at Harvard use complementary DNA in synthesis?

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

What is the purpose of tagging in combinatorial synthesis?

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

How do Harvard researchers use complementary DNA in synthesis?

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