845781-34-2Relevant academic research and scientific papers
Stereoselective synthesis of lower and upper rim functionalized tetra-α isomers of calix[4]pyrroles
Díaz-Moscoso, Alejandro,Hernández-Alonso, Daniel,Escobar, Luis,Arroyave, Frank A.,Ballester, Pablo
, p. 226 - 229 (2017)
Hydroxyaryl alkyl ketones with functionalized alkyl chains often fail to produce the corresponding tetra-α calix[4]pyrroles in Br?nsted acid mediated condensations with pyrrole. A remarkable effect exerted by the addition of methyltrialkylammonium chloride during the acid-mediated syntheses of a series of meso-(tetrahydroxyaryl)-meso-tetraalkylcalix[4]- pyrroles featuring alkyl terminal chloro or ester groups is reported. The ammonium salt enhances the cyclocondensation reaction and induces the almost exclusive formation of the tetra-α isomers.
Iridium-Catalyzed Asymmetric Hydrogenation of ?- A nd ?-Ketoacids for Enantioselective Synthesis of ?- A nd ?-Lactones
Hua, Yun-Yu,Bin, Huai-Yu,Wei, Tao,Cheng, Hou-An,Lin, Zu-Peng,Fu, Xing-Feng,Li, Yuan-Qiang,Xie, Jian-Hua,Yan, Pu-Cha,Zhou, Qi-Lin
supporting information, p. 818 - 822 (2020/02/15)
A highly efficient asymmetric hydrogenation of ?- A nd ?-ketoacids was developed by using a chiral spiro iridium catalyst (S)-1a, affording the optically active ?- A nd ?-hydroxy acids/lactones in high yields with excellent enantioselectivities (up to >99% ee) and turnover numbers (TON up to 100000). This protocol provides an efficient and practical method for enantioselective synthesis of Ezetimibe.
A 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - ketone (by machine translation)
-
Paragraph 0048; 0049; 0050, (2018/03/24)
The invention discloses a method for synthesizing 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - one method, its steps are: halogen anisole with glutaric anhydride reaction for the preparation of 5 - (3 - methoxyphenyl) - 5 - oxo-valeric acid, reducing 5 - (3 - methoxyphenyl) - 5 - oxo-valeric acid for the preparation of 5 - (3 - methoxyphenyl) pentanoic acid; 5 - (3 - methoxyphenyl) pentanoic acid through the intramolecular Friedel-crafts acylation reaction to obtain 2 - methoxy - 6, 7, 8, 9 - tetrahydrobenz cyclohepta - 5 - one. The method of the invention the synthesis step is short, low cost, the total yield is high, can be used for industrial production. (by machine translation)
Visible-Light-Promoted Metal-Free Aerobic Oxidation of Primary Amines to Acids and Lactones
Cheng, Xiaokai,Yang, Bo,Hu, Xingen,Xu, Qing,Lu, Zhan
supporting information, p. 17566 - 17570 (2016/11/29)
A unique metal-free aerobic oxidation of primary amines via visible light photocatalytic double carbon–carbon bonds cleavage and multi carbon–hydrogen bonds oxidation was observed. Aerobic oxidation of primary amines could be controlled to afford acids by using dioxane with 18 W CFL, and lactones by using DMF with 8 W green LEDs, respectively. A plausible mechanism was proposed based on control experiments. This observation showed direct evidences for the fragmentation in the aerobic oxidation of aliphatic primary amines.
Synthesis and cholinesterase activity of phenylcarbamates related to Rivastigmine, a therapeutic agent for Alzheimer's disease
Mustazza, Carlo,Borioni, Anna,Giudice, Maria Rosaria Del,Gatta, Franco,Ferretti, Rosella,Meneguz, Annarita,Volpe, Maria Teresa,Lorenzini, Paola
, p. 91 - 109 (2007/10/03)
In order to develop new cholinesterase agents effective against Alzheimer's disease (AD) we synthesized some phenylcarbamates structurally related to Rivastigmine and evaluated their in vitro and in vivo biological activity. Among the compounds which displayed the most significant in vitro activity, 1-[1-(3-dimethylcarbamoyloxyphenyl)ethyl]piperidine (31b), in addition to a simple and cheaper synthesis, showed lower toxicity and very similar therapeutic index in comparison with Rivastigmine.
