Description:
An invention to utilize “green chemistry” in a metal-free, mild condition to synthesize pharmaceutical agents.
The Invention
This invention is a powerful phosphorylation reagent called NHP-thiourea that can generate a phosphorus-carbon (P-C) bond and phosphorus-nitrogen (P-N) bond with metal-free reaction conditions. These P-C and P-N bonds are often present in pharmaceuticals and biologically active compounds. Current methods to generate a P-C bond utilize transition metal-catalyzed coupling reactions that requires additional steps for removal of metal impurities. The NHP-thiourea has been demonstrated as a reagent in 6 peer-reviewed publications to produce a various phosphonates.
Key Benefits
• Metal-free, mild reaction conditions
• Reduces number of synthetic steps
• Cost effective
• Environmentally friendly
Applications
• Reagent for synthesis of various phosphonates:
• Vinylphosphonates
• Hydrazine phosphonates
• α-Aminophosphonates
• α-Hydroxyphosphonates
• B-Aminophosphonates
• y-Ketophosphonates
Market Opportunity
Reducing the number of synthetic steps and removal of impurities such as toxic metal catalysts from drugs are challenging tasks within the pharmaceutical industry, and are significantly related to price deviations. The transition-metal-free synthetic route presents a green and cost-effective method.
Development Status
Gram quantities of the material have been prepared for characterization and testing. 15 plus different NHP-thiourea derivatives have been successfully synthesized.
Intellectual Property Status
Issued US Patent No. 10,633,403