No abstract

Bridged bicyclic morpholines are important building blocks in medicinal chemistry research. The bicyclic morpholine 6oxa-3-azabicyclo[3.1.1]heptane (2a) is of particular interest as a morpholine isostere because it is achiral and shows properties similar to that of morpholine based on a derived analogue. The first synthesis of morpholine 2a (tosylate salt) is described. The six-step sequence begins with inexpensive starting materials and uses straightforward chemistry.