abstract |
A novel process for the preparation of 2-azabicyclo-3-carboxylic acid hydrochloride of formula (I), by reacting the compound of formula (II) with an acylating agent in a non-polar solvent at 0-150 °C to give a compound of formula (III), which is reacted with an enamine of formula (IV) in a non-polar solvent in the presence of an organic base at 0 °C to 150 °C to yield a compound of formula (V), which is hydrolytically cyclised to give a compound of formula (VI) and further catalytically hydrogenated to give the compound of formula (I). |