166410-37-3Relevant academic research and scientific papers
Flow-mediated synthesis of Boc, Fmoc, and Dd iv monoprotected diamines
Jong, Thingsoon,Bradley, Mark
supporting information, p. 422 - 425 (2015/03/03)
A series of monoprotected aliphatic diamines (21 examples) were synthesized via continuous flow methods. The carbamates and enamines were obtained in 45-91% yields using a 0.5 mm diameter PTFE tubular flow reactor. Using readily accessible protecting group precursors, the procedure serves as an attractive alternative to existing batch-mode synthetic routes by providing direct, multigram access to N-Boc-, N-Fmoc-, and N-Ddiv-protected compounds with productivity indexes of 1.2-3.6 g/h.
New series of potent δ-opioid antagonists containing the H-Dmt-Tic-NH-hexyl-NH-R motif
Li, Tingyou,Shiotani, Kimitaka,Miyazaki, Anna,Fujita, Yoshio,Tsuda, Yuko,Ambo, Akihiro,Sasaki, Yusuke,Jinsmaa, Yunden,Marczak, Ewa,Bryant, Sharon D.,Lazarus, Lawrence H.,Okada, Yoshio
, p. 5517 - 5520 (2007/10/03)
Heterodimeric compounds H-Dmt-Tic-NH-hexyl-NH-R (R = Dmt, Tic, and Phe) exhibited high affinity to δ- (Kiδ = 0.13-0.89 nM) and μ-opioid receptors (Kiμ = 0.38-2.81 nM) with extraordinary potent δ antagonism (pA2 = 10.2-10.4). These compounds represent the prototype for a new class of structural homologues lacking μ-opioid receptor-associated agonism (IC50 = 1.6-5.8 μM) based on the framework of bis-[H-Dmt-NH]-alkyl (Okada, Y.; Tsuda, Y.; Fujita, Y.; Yokoi, T.; Sasaki, Y.; Ambo, A.; Konishi, R.; Nagata, M.; Salvadori, S.; Jinsmaa, Y.; Bryant, S. D.; Lazarus, L. H. J. Med. Chem. 2003, 46, 3201), which exhibited both high μ affinity and bioactivity.
