76465-01-5Relevant academic research and scientific papers
Relaying asymmetry of transient atropisomers of o-iodoanilides by radical cyclizations
Petit, Marc,Lapierre, Andre J. B.,Curran, Dennis P.
, p. 14994 - 14995 (2005)
Atropisomers of N-2°-alkyl-N-acryloyl-2-iodoanlides have been resolved by chromatography and crystallization-induced asymmetric transformation. These molecules have atropisomerization barriers of 23-24 kcal/mol and return to equilibrium ratios over severa
Photoinduced [3+2] Annulation of Alkene with o-Iodoanilines: An Expedient Approach to Indolines
Zhao, Xinxin,Guo, Lin,Yang, Chao,Xia, Wujiong
supporting information, p. 1341 - 1348 (2020/11/19)
A highly regioselective [3+2] cyclization of alkenes with 2-iodoanilines under the irradiation of UV light is described. This general, metal-free strategy facilitates the direct preparation of 2-mono-/disubstituted indolines as well as spiroindolines through alkene carboamination in one step. Mechanistic studies suggested that the photochemical protocol proceeded via a radical pathway.
Synthesis of C4-Aminated Indoles via a Catellani and Retro-Diels-Alder Strategy
Zhang, Bo-Sheng,Li, Yuke,Zhang, Zhe,An, Yang,Wen, Yu-Hua,Gou, Xue-Ya,Quan, Si-Qi,Wang, Xin-Gang,Liang, Yong-Min
supporting information, p. 9731 - 9738 (2019/06/24)
Highly functionalized 4-aminoindoles were synthesized via the three-component cross-coupling of o-iodoaniline, N-benzoyloxyamines, and norbornadiene. The Catellani and retro-Diels-Alder strategy was used in this domino process. o-Iodoaniline, with electron-donating and sterically hindered protecting groups, made the reaction selective toward o-C-H amination. On the basis of density functional theory calculations, the intramolecular Buchwald coupling of this reaction underwent a dearomatization and a 1,3-palladium migration process. The reasons for the control of the chemical selectivity by the protecting groups are given. Moreover, synthetic applications toward 4-piperazinylindole and a GOT1 inhibitor were realized.
Synthesis of C4-Aminated Indoles via a Catellani and Retro-Diels-Alder Strategy
Zhang, Bo-Sheng,Li, Yuke,Zhang, Zhe,An, Yang,Wen, Yu-Hua,Gou, Xue-Ya,Quan, Si-Qi,Wang, Xin-Gang,Liang, Yong-Min
supporting information, (2019/06/24)
Highly functionalized 4-aminoindoles were synthesized via the three-component cross-coupling of o-iodoaniline, N-benzoyloxyamines, and norbornadiene. The Catellani and retro-Diels-Alder strategy was used in this domino process. o-Iodoaniline, with electron-donating and sterically hindered protecting groups, made the reaction selective toward o-C-H amination. On the basis of density functional theory calculations, the intramolecular Buchwald coupling of this reaction underwent a dearomatization and a 1,3-palladium migration process. The reasons for the control of the chemical selectivity by the protecting groups are given. Moreover, synthetic applications toward 4-piperazinylindole and a GOT1 inhibitor were realized.
BIARYL DERIVATIVES AS GPR120 AGONISTS
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Paragraph 848; 863; 864; 865, (2015/01/16)
The present invention relates to biaryl derivatives of Formula 1, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The biaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in the liver or in muscle due to anti-inflammatory action in macrophages, lipocytes, etc., and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, obesity, non-alcoholic fatty liver, steatohepatitis, osteoporosis or inflammation.
Amines useful as brain imaging agents
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, (2008/06/13)
Certain radioiodine containing amines useful as brain imaging agents are disclosed. The compounds of the invention are represented by the formula STR1 wherein I is a radioisotope of iodine with I-123 being preferred, R is lower alkyl or halogen, R1 and R2 are the same or different and are selected from the group consisting of hydrogen and lower alkyl, R3 and R4 are the same or different and are selected from the group consisting of hydrogen, alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl and substituted carbamoyl methyl or R3 and R4 taken together with the nitrogen to which they are attached form a 5- or 6-membered ring which may be substituted with one or more lower alkyl groups, x is 0 to 4, y is 0 to 3 and z is 0 or 1 and pharmaceutically acceptable acid addition salts thereof.
