A series of heterocyclic cycloalkanol ethylamines have been prepared to expand our norepinephrine reuptake inhibitor (NRI) program. Synthesis of a variety of heterocycles identified (+)-S-21, a potent NRI efficacious in an animal model for thermoregulatory dysfunction.
[Young, Jonathan R.; Huang, Song X.; Chen, Irene; Walsh, Thomas F.; DeVita, Robert J.; Wyvratt Jr., Matthew J.; Goulet, Mark T.; Ren, Ning; Lo, Jane; Yang, Yi Tien; Yudkovitz, Joel B.; Cheng, Kang; Smith, Roy G. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 15 p. 1723 - 1727]
[Young, Jonathan R.; Huang, Song X.; Chen, Irene; Walsh, Thomas F.; DeVita, Robert J.; Wyvratt Jr., Matthew J.; Goulet, Mark T.; Ren, Ning; Lo, Jane; Yang, Yi Tien; Yudkovitz, Joel B.; Cheng, Kang; Smith, Roy G. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 15 p. 1723 - 1727]