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Custom Chemicals

Peptide Synthesis

Peptide synthesis technology(SYNCSOL®)

SYNCSOL

We have been conducting research on the manufacturing of peptide compounds by solid-phase and liquid-phase synthesis. We have especially been focusing on the development of new liquid-phase synthesis methods for peptides, we were able to establish a unique liquid-synthesis platform (SYNCSOL®). SYNCSOL® is a peptide manufacturing technology that consists of both silyl protection technology (SIPS®) and unprotected amino acid condensation (R-Coupling®). High quality peptide fragments can be synthesized and production of high purity target compounds by convergent liquid-phase peptide synthesis is made possible by using this platform. With this platform, we achieved a major reduction in the raw materials used together with the improvement of peptide quality before purification, leading to the reduction of purification effort. We are able to propose a price competitive synthesis method for every peptide compound through the use of SYNCSOL®.

Here are the descriptions for the two core technologies that was used to realize SYNCSOL®:

SIPS® (technology using silyl protective groups) a)

SIPS® is one of our original liquid-phase synthesis method. By protecting the carboxyl terminus (C-terminus) by silyl groups, side reactions are suppressed and physical characteristics are improved, thereby enabling the attainment of high-quality peptide intermediates through just liquid separation or crystallization.

SIPS™ (Technology by using Silyl protective group) a

Silyl protective groups have the following features:

  • (1)Free strategies for synthesis: As silyl groups can be used for peptide synthesis in conjunction with Fmoc group, Coc group or Cbz group (commonly used for protection of amino groups), which enables us to provide various solutions from different approaches for synthesis of “difficult” amino acids sequences.
  • (2)Suppression of side reactions: Dipeptide cyclization is an issue in liquid-phase synthesis, but our technology is able to suppress it and realize a high-efficiency synthesis of high-purity peptides.
  • (3)Selective deprotection: Since selective deprotection without influencing the side chain protective groups or peptide purity is possible, our technology has the optimal feature for manufacturing high-quality peptides.

R-Coupling™ (Technology to extend peptides from N-terminal using non-protective amino acids) b

R-Coupling® (technology to elongate peptides from N- terminus using unprotected amino acids) b)

Traditional methods for peptide synthesis elongated peptides only to N-terminus by sequential condensation from C-terminus (carboxyl-terminus) to N-terminus (amino-terminus), from the viewpoint of avoiding epimerization risks. However, Nissan Chemical Corporation was successful in developing an unprecedented technology of R-Coupling® which enabled the elongation of peptides in the N- to C-direction.

R-Coupling® has the following features:

  • (1)By using our original technology that combines our new bulky condensing agent ISTA-X and silylating agent, amino acids having both amino-terminus and carboxyl-terminus unprotected can be used as raw materials. As deprotection processes are not required, the steps required in peptide synthesis can be shortened.
  • (2)Condensation of low reactive N-substituted amino acids is possible by using ISTA-X as the agent, which has a high reactivity and is suppressive of side reactions, this method can be applied to special peptides such as N-substituted amino acids and other unnatural amino acids.

R-Coupling® can reduce material costs using, for example, natural amino acids without protective groups as raw materials. Also, in addition to the conventional peptide elongation from the N-terminus, peptides may be elongated from the C-terminus, which allows us to offer versatile synthetic strategies that were not possible through conventional peptide synthesis methods. As a result, we are able to realize a high-quality, cost-reduced peptide synthesis even for amino acid sequences that were said to be difficult to synthesize.

  • a)WO 2019069978, WO 2020162393
  • b)WO 2020162393, WO 2020189621, Organic Lett., 2020, 22, 8039
    Synfacts 2021, 17, 103 (Synfacts of the month)
    Org. Process Res. Dev. 2021, 25, 2029–2038

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