Platform for Multiple Isotope Labeling via Carbon-Sulfur Bond Exchange

Area of Science:

• Organic Chemistry
• Isotope Chemistry
• Medicinal Chemistry

Background:

• Isotopes are crucial for life science applications like nuclear imaging and pharmaceutical profiling.
• Current isotope insertion methods are element-specific and challenging.
• Sulfur isotope labeling is underexplored despite sulfur's prevalence in bioactive molecules.

Purpose of the Study:

• To develop a novel strategy for selective sulfur isotope exchange.
• To overcome limitations of element-specific isotope labeling.
• To create a versatile platform for multiple isotope labeling.

Main Methods:

• Nickel-catalyzed reversible carbon-sulfur (C-S) bond activation.
• Application of the strategy to various isotopes including deuterium, carbon-13, sulfur-34, and carbon-14.
• Testing compatibility with diverse organic substrates, including pharmaceuticals.

Main Results:

• Achieved selective sulfur isotope exchange using the developed method.
• Demonstrated the platform's applicability to multiple isotopes (H, C, S).
• Confirmed compatibility with a wide range of pharmaceutical compounds.
• Showcased potential for isotopic encryption of organic molecules.

Conclusions:

• The nickel-catalyzed C-S bond activation provides a unique platform for versatile isotope labeling.
• This method expands the possibilities for sulfur isotope labeling in organic chemistry and drug development.
• The technology holds promise for advanced applications such as isotopic encryption.