Peptide Coupling Reagents

All kinds of peptide coupling reagents are available from stock, High purity and reliable quality.

The global demand for high-efficiency and low-toxic drugs has established a broad market for peptide drug research and development. The peptide drugs has become an indispensable and important field of modern drug research and development, and its development is getting faster and faster. In the development of peptide drugs, chemical synthesis is an important method for the research and synthesis of peptide drugs. Peptide coupling reagents are special chemical reagents that are indispensable for the construction of amide bonds in peptide synthesis. High-efficiency peptide coupling reagents have always been a research hotspot in the field of peptides development .

At present, there are many commercial peptide coupling reagents, but the condensing agents which are more influential and widely used are mainly divided into carbodiimide type, phosphorus cation type and urea cation type from the perspective of molecular structure.

1.Carbodiimide

DCC is the first carbodiimide type of coupling reagent developed in 1955. So far, DCC is still one of the most commonly used peptide condensing agents in peptide synthesis. In order to reduce the by-products produced by the reaction, the DCC structure has been improved, and some carbodiimide-type coupling reagent that generate water-soluble reaction by-products have been developed, such as DIC, EDC and BDDC, etc.

The peptide coupling reagents obtained by immobilizing the carbodiimide on the polymer makes the post-treatment of the reaction easier, such as resin immobilized EDC (P-EDC). This type of condensing agent is suitable for the large-scale production of peptides. It is usually used together with additives such as HOSu, HOBt, HOAt, or HOOBt to inhibit the racemization of the product, and it can also effectively inhibit the formation of by-products such as N-acylurea. HOBt is the most widely used among them. DCC-HOBt compound peptide coupling reagent has become one of the most widely used condensation methods. HOOBt can inhibit racemization more effectively than HOBt. HOAt is a new additive that has only been developed in recent years. It can not only effectively inhibit racemization, but also greatly increase the reaction speed. It is especially suitable for the synthesis of sterically hindered peptides.

Carbodiimide-type high-purity condensing agent available from Omizzur Biotech

2.Phosphorus

The use of acylphosphorus cations as active intermediates for the formation of amide bonds was first proposed by Kenner in 1969 and this method was used for peptide synthesis. In 1975, Castro designed and synthesized another HOBt-based phosphorus positive ion peptide coupling reagent, BOP, which is widely used in the solid-phase and liquid-phase synthesis of peptides. Later, PyBOP, a condensation agent with low by-product toxicity and relatively higher reactivity, was developed and commercialized.

Later developed HOAt-based phosphorus cations and -halogenated phosphorus cations type condensing agents such as AOP, PyAOP, BrOP, PyClOP, PyBrOP and so on. These condensing agents can efficiently promote the formation of sterically hindered amide bonds, and are widely used in the synthesis of bioactive peptides ,rich in N-methyl amino acids or C,C-dialkylated amino acids.

Phosphorus type high-purity coupling reagents available from Omizzur Biotech

3.Urea cation

In 1978, Dourtoglou successfully used HOBt-based urea cation HBTU in peptide synthesis. This type of peptide coupling reagents has been developed rapidly and has developed a series of products: TBTU, HBPyU, HBPipU, HBMDU, HATU, HAPyU, HAMDU, TAPipU, HDTU, HPyOPfp, HPySPfp, HAPyTU, TOTU, HAPipU. These condensing agents all show good performance in peptide synthesis, and have many advantages such as fast reaction speed, small product racemization, and high yield, especially reagents based on HOBt and HOAt. Among them, the HOAt-based urea positive ion condensing agent can effectively promote the formation of sterically hindered amide bonds.

Among these coupling reagents, TBTU, HATU, PyCIU, TFFH, BTFFH, CIP, and CTDP are widely used, and they have been successfully used in peptides containing N-methyl amino acids and C, C-dialkylated amino acids in peptide synthesis.

Urea cation type high-purity coupling reagents available from Omizzur Biotech

4.Other peptide coupling reagents

Other types of condensing agents: In addition to the above-mentioned major types of condensing agents, some other types of condensing agents also have a certain degree of application in peptide synthesis. The representative ones are: BOP-Cl, FDP, FDPP, DEPBT, EDQ etc. Among them, BOP-Cl can efficiently promote the formation of sterically hindered amide bonds with less racemization, and has been successfully used in the synthesis of bioactive peptides rich in N-methyl amino acids.

FDPP is particularly suitable for the synthesis of cyclic peptides. DEPBT is a HOBt-derived phosphate ester, which is characterized by less racemization of the product. EEDQ is a classic condensing agent. It mainly promotes the synthesis of peptides by forming mixed anhydride intermediates, but the product needs to pay attention to racemization.

Other Type of peptide coupling reagents

Omizzur Biotech specializes in various peptide coupling reagents, group protecting agents, various protected amino acid spot supply and peptide synthesis, custom peptide library  services. If you have any product requirements, please send an email to the customer service center ( left side of website ). We will provide you with the latest product quotation within 2h.