Imidazole-1-sulfonyl azide HCl (Synthonix compound I1899) is an efficient, inexpensive, and shelf-stable diazotransfer reagent.
It has proven to equal triflyl azide in its ability to act as a "diazo donor" in the conversion of both primary amines into azides and activated methylene substrates into diazo compounds.
Most importantly it is inexpensive, shelf-stable, and conveniently crystalline.
The Oxetane ring is a good isoteric replacement for methylene and gem dimethyl motifs for improving key physicochemical parameters to assist property guided drug discovery. Introduction of oxetane motifs at different locations has been shown to:
- Improve the physico- and biochemical properties for the active scaffold
- Enhance solubility, reduce lipophilicity, amphiphilicity, and hERG liability
- Impart robust chemical stability under various acidic and basic conditions
- Improve resistance towards metabolic degradation
Recent improvements have allowed Synthonix to substantially reduce the price of 3-Oxetanone:
1g: $58 5g: $250 25g: $900 100g: $2900