1-Hydroxybenzotriazole Hydrate丨CAS 123333-53-9

Applications

1. Peptide Synthesis Coupling Reagent Additive

1-Hydroxybenzotriazole hydrate丨CAS 123333-53-9 is widely used as an additive in peptide coupling reactions, particularly alongside carbodiimide reagents like Dicyclohexylcarbodiimide (DCC) or EDC (1-ethyl-3-(3-dimethylaminopropyl)carbodiimide).

It suppresses racemization and increases the efficiency and yield of peptide bond formation by stabilizing reactive intermediates.

2. Activation of Carboxyl Groups

Facilitates the formation of active esters from carboxylic acids, which react readily with amines to form amides or peptides.

Helps in amide bond formation in pharmaceuticals and fine chemicals synthesis.

3. Synthesis of Complex Organic Molecules

Used in the preparation of small molecules and complex natural products requiring efficient amide or ester bond formation.

A key reagent in medicinal chemistry for assembling drug candidates and biologically active compounds.

4. Reduction of Side Reactions

Helps reduce side reactions such as N-acylurea formation, which are common when carbodiimides are used alone.

Benefits

1. Racemization Suppression

HOBt significantly lowers the risk of racemization during peptide bond formation, preserving the stereochemistry of amino acids and improving product purity.

2. Improved Coupling Efficiency

Forms more reactive and stable intermediates than carbodiimides alone, leading to higher coupling efficiency and yields.

3. Versatile and Widely Compatible

Compatible with a wide variety of amino acids and peptide synthesis protocols (both solution-phase and solid-phase).

4. Enhanced Safety Compared to Anhydrous HOBt

The hydrate form of HOBt is considered safer and less prone to explosive hazards than anhydrous HOBt, improving handling safety in laboratories and industry.

Summary

1-Hydroxybenzotriazole hydrate丨CAS 123333-53-9 is a key additive in peptide synthesis and organic coupling reactions, valued for its ability to increase coupling efficiency, reduce racemization, and enhance product purity. It is widely used in pharmaceutical and research labs for assembling peptides and complex molecules under safer and more efficient conditions.