Heather Torgerson, & Dr. Thomas Schulze
Neurosciences (Central Nervous System, CNS) Research & Development (R&D) is a modern field of study with pivotal implications in the pursuit of novel pharmacological studies. Currently available anti-psychotic drugs (aka: Risperidone, Paliperidone) contain 6-Membered Piperidine & Piperazine ring systems which are well-established central pharmacophore systems likely responsible for biological action. Their highly unfavorable side-effect profile is mainly attributed to an enormous amount of Off-Target biological actions, here hypothesized by very high degree of conformational freedoms exerted my 6-Membered Ring Systems. It is hypothesized that conformationally flexible substituted 6-Membered Piperidine ring systems may potentially be responsible for Off-Target biological activity. The research objective is to synthesize conformationally constrained 5- Membered Proline-Based Diamine Analogues. By using Trans-Hydroxy-4-L-Proline as the starting molecule, the diamine analogue is planned to be synthesized in 6 steps. The first 2 synthetic steps have been completed, using small quantities initially and then repeating at larger multi-gram scale. The diamine synthesis is planned to be governed by Lipinski’s Rule-of-Five considerations.