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Synthetic methods used in Combinatorial Chemistry

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Synthetic methods used in Combinatorial Chemistry

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2. Parallel synthesis:

Each starting material is reacted with each building block separately.

The product is split into ‘n’ portions before it is reacted with n new building blocks.

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Synthetic methods used in Combinatorial Chemistry

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Synthetic methods used in Combinatorial Chemistry

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1. Split and mix synthesis or Split and pool synthesis or Portioning – Mixing synthesis:

Starting material is split in ‘n’ portions, reacted with ‘n’ building blocks.

Recombined in one flask.

This procedure is repeated.

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Types of combinatorial synthesis

2)Solution phase combinatorial chemistry:

Conducting chemical reaction simultaneously.

Most ordinary synthetic chemistry takes place in solution phase.

In solution phase used 2 vehicles-

PEG

Liquid Teflon

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Rink amide resin

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Merrifield resin

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Types of combinatorial synthesis

1)Solid phase combinatorial chemistry.

starting compound is attached to an insoluble resin bead.

Reagents are added to the solution in excess.

products can be isolated by simple filtration.

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Connection between structure and reactivity

Way to build organic compounds from smaller entities

Have enables the discovery of many breakthrough therapies.

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Goal of Synthetic Chemistry

Enhance structural diversity

Developing a probe

Developing lead molecule

Enhance understanding of biological targets

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Asymmetric hydrogenetion

Asymmetric epoxidation

Combinatorial method

Pd-catalyzed cross couplings

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Principle:

Prepare a large number of different compounds.

Identify the most promising compound.

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1.   Making a library.

collection of the finally synthesized compounds.

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2.  Finding the active compound.

Screening mixtures for biological activity