Combinatorial Chemistry


It is a method of preparation of a large number of compounds in a single process, libraries can be made either as a mixture or individual compounds which are developed by computer software. Techniques that are utilized for the identification of library components. These can be used for different fields. Combinatorial Chemistry is a new method developed to reduce the time and cost of producing effective, marketable, and competitive new drugs. Combinatorial Chemistry is used to create large numbers of molecules that can be detected efficiently. This technique is useful in many areas such as Pharmaceutical chemistry, Biotechnology, and Agrochemistry. Combinatorial chemistry is a technique by which huge numbers of different but structurally similar molecules are produced rapidly and screened for pharmacological assay. In this technique, large numbers of analogs are produced using the same reaction vessel and reaction conditions. By producing more diverse compound libraries, companies increase the probability that they will find novel compounds of significant therapeutic and commercial value. The combinatorial approach can give rise to millions of compounds in the same time compared to the traditional method of synthesis which produces only one compound at a time.


It is not so old concept, it had been taken industry in1990, but it was started in 1960 as Merrifield suggested solid-state synthesis. Initially, this technique applied to synthesis oligonucleotide and peptides. In 1984, pin-shaped solid support discovered by Geysen and he announced that he and his team made an encoding technique in which tags are connected via linkers.

Although its roots are from the 1960s it came into existence in 1990. Many modern techniques have been applied to get pure compounds in combinatorial synthesis.


  • A very fast technique to develop many compounds at the same time.
  • Economical as it requires fewer efforts.
  • A quite easy process.
  • More chances to discover a drug.
  • Drug optimization can be done.


  • Efficiency gets affected by the size, solubility and functional group.
  • Achiral molecules tend to produce.
  • Assay material wastage.
  • Limited structure variation.
  • Less probability of finding samples.