37787-77-2Relevant articles and documents
Modular Synthesis of Carbazole-Substituted Phthalimides as Potential Photocatalysts
F?ldesi, Tamás,Gonda, Zsombor,Nagy, Bálint,Novák, Zoltán
supporting information, (2021/11/22)
The modular synthesis of carbazole functionalized phthalimides (PIs) and their applicability as catalyst in selected photocatalytic transformations are reported. The developed synthetic approach provides high variability of phthalimide considering that the synthesis of the phthalimide core can be easily performed. Starting from fluorophthalic acid anhydrides, the corresponding fluorophthalimides were prepared with various amines, and the fluoro function ensured the introduction of carbazoles into the phthalimide framework through aromatic nucleophilic substitution. Besides the synthetic developments, some of the carbazolyl phthalimides were tested in four different photocatalytic transformations, which showed attractive and comparable activity to the known 4-CzIPN and noble metal complexes.
Synthesis and evaluation of in Vivo anti-hypothermic effect of the N- And C-terminus modified thyrotropin-releasing hormone mimetic: [(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)-carbonyl]-[3-(thiazol-4-yl)-L-alanyl]-L-prolinamide
Kobayashi, Naotake,Sato, Norihito,Sugita, Katsuji,Kihara, Tsuyoshi,Koike, Katsumi,Sugawara, Tamio,Tada, Yukio,Yoshikawa, Takayoshi
, p. 314 - 324 (2021/04/30)
We explored orally effective thyrotropin-releasing hormone (TRH) mimetics, which show high central nervous system effects in structure–activity relationship studies based on in vivo antagonistic activity on reserpine-induced hypothermia (anti-hypothermic effect) in mice starting from TRH. This led us to the TRH mimetic: [(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-[3-(thiazol-4-yl)-L-alanyl]-L-prolinamide 1, which shows a higher anti-hypothermic effect compared with that of TRH after oral administration. We next attempted further chemical modification of the N- and C-terminus of 1 to find more orally effective TRH mimetics. As a result, we obtained several N- and C-terminus modified TRH mimetics which showed high anti-hypothermic effects.
A Ni–Ir Dual Photocatalytic Liebeskind Coupling of Sulfonium Salts for the Synthesis of 2-Benzylpyrrolidines
Varga, Bálint,Gonda, Zsombor,Tóth, Balázs L.,Kotschy, András,Novák, Zoltán
, p. 1466 - 1471 (2019/11/03)
A new method has been developed for the synthesis of 2-benzylpyrrolidines utilizing cross-coupling and photoredox catalysis. Using a well-established dual Ni–Ir system, we were able to successfully couple benzylsulfonium salts with proline utilizing radical forming through CO2 extrusion. This enabled the simple one-step synthesis of 2-benzylpyrrolidines from stable, inexpensive starting materials.