128577-66-2Relevant academic research and scientific papers
Stereospecific Alkene Aziridination Using a Bifunctional Amino-Reagent: An Aza-Prilezhaev Reaction
Farndon, Joshua J.,Young, Tom A.,Bower, John F.
supporting information, p. 17846 - 17850 (2019/01/04)
In situ deprotection (TFA) of O-Ts activated N-Boc hydroxylamines triggers intramolecular aziridination of N-tethered alkenes to provide complex N-heterocyclic ring systems. Synthetic and computational studies corroborate a diastereospecific aza-Prilezhaev-type mechanism. The feasibility of related intermolecular alkene aziridinations is also demonstrated.
Asymmetric organocatalytic synthesis of complex cyclopenta[ b ]quinoline derivatives
Jensen, Kim L.,Dickmeiss, Gustav,Donslund, Bjarke S.,Poulsen, Pernille H.,Jorgensen, Karl Anker
supporting information; experimental part, p. 3678 - 3681 (2011/08/22)
An efficient one-pot procedure that provides a direct access to polycyclic hexahydrocyclopenta[b]quinoline derivatives having five stereogenic centers has been developed. The system displays great tolerance toward different aldehydes, anilines, and nitroa
Trisubstituted benzene leukotriene B4 receptor antagonists: Synthesis and structure-activity relationships
Konno, Mitoshi,Nakae, Takahiko,Sakuyama, Shigeru,Odagaki, Yoshihiko,Nakai, Hisao,Hamanaka, Nobuyuki
, p. 1649 - 1674 (2007/10/03)
A series of trisubstituted benzenes which demonstrate leukotriene B4 (LTB4, 1) receptor affinity was prepared. Previous trisubstituted benzenes from our laboratory showed high affinity to the LTB4 receptor but demonstrated
Benzophenone Dicarboxylic Acid Antagonists of Leukotriene B4. 2. Structure-Activity Relationships of the Lipophilic Side Chain
Gapinski, D. Mark,Mallett, Barbara E.,Froelich, Larry L.,Jackson, William T.
, p. 2807 - 2813 (2007/10/02)
A series of lipophilic benzophenone dicarboxylic acid derivatives were found to inhibit the binding of the potent chemotoxin leukotriene B4 (LTB4) to its receptor on intact human neutrophils.Activity at the LTB4 receptor was determined by using a 3H>LTB4-binding assay.The structure-activity relationship for the lipophilic side chain was systematically investigated.Compounds with n-alkyl side chains of varying lengths were prepared and tested.Best inhibition of 3H>LTB4 binding was observed with the n-decyl derivative.Analogues with alkyl chains terminated with an aromatic ring showed improved activity.The 6-phenylhexyl side chain was optimal.Substitution on the terminal aromatic ring was also evaluated.Methoxyl, methylsulfinyl, and methyl substituents greatly enhanced the activity of the compound.For a given substituent, the para isomer had the best activity.Thus the nature of the lipophilic side chain can greatly influence the ability of the compounds to inhibit the binding of LTB4 to its receptor on intact human neutrophils.The most active compound from this series, 84 (LY223982), bound to the LTB4 receptor with the affinity approaching that of the agonist.
