49761-82-2Relevant articles and documents
A highly selective, one-pot multiple-addition convergent synthesis of polycarbonate dendrimers [3]
Rannard,Davis
, p. 11729 - 11730 (2000)
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Probing the mid-gorge of cholinesterases with spacer-modified bivalent quinazolinimines leads to highly potent and selective butyrylcholinesterase inhibitors
Chen, Xinyu,Tikhonova, Irina G.,Decker, Michael
, p. 1222 - 1235 (2011)
The spacer structure of homobivalent quinazolinimes acting as potent acetyl-(AChE)- and butyrylcholinesterase (BChE) inhibitors was chemically modified introducing tertiary amine and acyl-amide moieties, and the activities at both ChEs were evaluated. Molecular docking was applied to explain the data and probe the capacity of the mid-gorge site of both ChEs. The novel spacer structures considerably alter the biological profile of bivalent quinazolinimines with regard to both inhibitory activity and selectivity. Mutual interaction of binding to the various sites of the enzymes was further investigated by applying also different spacer lengths and ring sizes of the alicycle of the tricyclic quinazolinimines. In order to achieve selectivity toward BChE and to improve inhibitory activities, the spacer structure was optimized and identified a highly potent and selective BChE inhibitor.
Enantioselective Syntheses of Strychnos and Chelidonium Alkaloids through Regio- and Stereocontrolled Cooperative Catalysis
Fyfe, James W. B.,Hutchings-Goetz, Luke S.,Snaddon, Thomas N.,Yang, Chao
supporting information, p. 17556 - 17564 (2020/08/14)
We describe enantioselective syntheses of strychnos and chelidonium alkaloids. In the first case, indole acetic acid esters were established as excellent partner nucleophiles for enantioselective cooperative isothiourea/Pd catalyzed α-alkylation. This provides products containing indole-bearing stereocenters in high yield and with excellent levels of enantioinduction in a manner that is notably independent of the N-substituent. This led to concise syntheses of (?)-akuammicine and (?)-strychnine. In the second case, the poor performance of ortho-substituted cinnamyl electrophiles in the enantioselective cooperative isothiourea/Ir catalyzed α-alkylation was overcome by appropriate substituent choice, leading to enantioselective syntheses of (+)-chelidonine, (+)-norchelidonine, and (+)-chelamine.
Preparation method of (2-methylamine-ethyl)-tert-butyl carbamate
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Paragraph 0024; 0026; 0028, (2019/07/01)
The invention discloses a preparation method of (2-methylamine-ethyl)-tert-butyl carbamate, and belongs to the technical field of organic chemical synthesis. The preparation method comprises followingsteps: 1, imidazole is dissolved in dichloromethane, and di-tert-butyl dicarbonate ester is added at room temperature, reaction is carried out for 2 to 3h at room temperature, and water washing drying are carried out so as to obtain an intermediate; and 2, the intermediate is dissolved in toluene, N-methylethylenediamine is added, an obtained mixture is heated to 60 to 70 DEG C, reaction is carried out for 2 to 4h, reduced pressure distillation is carried out to remove toluene, and purification is carried out so as to obtain (2-methylamine-ethyl)-tert-butyl carbamate. The operation steps arefew; by-product content is reduced with ensured (2-methylamine-ethyl)-tert-butyl carbamate synthesis yield; cost is relatively low; and batch production requirements are satisfied.