Synthesis and Properties of 2-Oxa-6-azaspiro[3.3]heptane Sulfonate Salts
An improved synthesis of the bicyclic spiro compound 2-oxa-6-azaspiro[3.3]heptane is presented. While this compound is often isolated as an oxalate salt, its isolation as a sulfonic acid salt yields a more stable and more soluble product. With these improved properties access to a wider range of reaction conditions with the spirobicyclic 2-oxa-6-azaspiro[3.3]heptane has been enabled.
Van Der Haas, Richard N. S.,Dekker, Jeroen A.,Hassfeld, Jorma,Hager, Anastasia,Fey, Peter,Rubenbauer, Philipp,Damen, Eric
p. 2394 - 2401
(2017/05/22)
The Development of a Manufacturing Route to an MCHr1 Antagonist
Process development work to provide an efficient manufacturing route to a MCHr1 antagonist is presented herewith. Features of this development work include a scalable manufacturing route to the useful 6-oxa-2-azaspiro[3.3]heptane building block and the use of a (soluble) alternative to sodium triacetoxyborohydride.