Description:
Novel cost-effective, metal-free synthetic method for β-aminophosphonates and α-aminophosphonates.
The Invention
This technology is a novel synthetic method towards β-aminophosphonates and α-aminophosphonates which are commonly found in pharmaceuticals and biologically active compounds. These are produced by using N-heterocyclicphosphine-thioureas (NHP-thiourea). This synthesis allows the formation of a P-C bond under metal-free, mild conditions.
Key Benefits
- Metal-free synthesis
- “Green Reaction” (reduces use of hazardous substances)
- Reaction can be completed under mild conditions
- Cost-effective
- Environmentally friendly
Applications
- Pharmaceutical
- Medicinal chemistry
- Agrochemistry
rket Opportunity
β-aminophosphonates and α-aminophosphonates are used as reagents to synthesize various phosphonates. Thus, they have several markets including active pharmaceutical ingredients, specialty chemical, and pesticide manufacturing.
The active pharmaceutical ingredients global market was $299.2 billion in 2020 and is forecasted to grow by a CAGR of 7.98% to $521.1 billion by 2030. The specialty chemical global market size was $588.2 billion in 2020 and is expected to grow at a CAGR of
6.17% up to $894.1 billion by 2028. The U.S. pesticide manufacturing market is currently $16.8 billion and is expected to grow at a CAGR of 1.4% to $17.9 billion by 2028.
In pharmaceutical industries, removal of impurities is a challenging task and significantly related to the price of drugs. Although this green method may be slower than other methods, it is a less hazardous cost-effective method.
Development and Intellectual Property Status
29 novel-aminophosphonates were synthesized using this method. Proof-of-principal has been performed with α-aminophosphonates, with the intention of screening various
substituted aziridines to explore the scope of electrophiles. Preliminary data suggests the synthesis of 2nd generation NHPs should be possible.