Formylation is an integral part of organic, medicinal and biological chemistry both in industrial and academic set-ups.
Current formylating procedures suffer a number of disadvantages:
- formic halides and formic anhydrides, tend to suffer from stability problems and are easily degraded upon storage.
- cyanomethyl formate is a very useful reagent, although it is difficult to prepare.
- isopropenyl formate is a very fast and efficient reagent, but its synthesis requires a multi-step sequence.
- coupling agents have also been used in conjunction with formic acid to achieve N- and O-formylation, however, the removal of the side products derived from the coupling agents is often labour intensive.
N-formyl benzotriazole is a stable and convenient reagent to achieve quick and efficient N- and O- formylation of alcohols, amines and even amides in mild and selective manner. The main challenge is the synthesis of N-formyl benzotriazole and its purification from the amount of urea by products.
Our patent protected synthesis of N-formyl benzotriazoles offers a product with much greater yield and higher purity compared to any previously known syntheses. The N-formyl benzotriazole is obtained by reacting a benzotriazole compound with a formyl anhydride.
A patent for this synthetic procedure was filed on 21 December 2010.
This technology is available as an Easy Access IP deal, available to companies and individuals to license for FREE.