77987-49-6Relevant articles and documents
Preparation method of N-(2-aminoethyl) morpholine
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Paragraph 0062-0064; 0073-0075, (2021/04/21)
The invention provides a preparation method of N-(2-aminoethyl) morpholine, which comprises the following steps: S1, adding ethanolamine into dichloromethane to fully dissolve, dropwise adding benzyl chloroformate into the solution, and reacting under alkaline conditions to generate an intermediate 1; S2, adding the intermediate 1 into dichloromethane, fully dissolving, dropwise adding 4toluenesulfonyl chloride, and reacting under an alkaline condition to generate an intermediate 2; S3, adding the intermediate 2 into acetonitrile to be fully dissolved, adding morpholine into the acetonitrile to generate an intermediate 3, wherein the structural formula of the intermediate 3 is shown as the following formula (3); and S4, adding the intermediate 3 into methanol, fully dissolving, and carrying out a catalytic hydrogenation reaction under the action of a catalyst to generate N-(2-aminoethyl)morpholine. According to the N-(2-aminoethyl)morpholine preparation method provided by the embodiment of the invention, the raw materials used in the reaction are cheap and easily available, the toxicity is low, the operation is simple and convenient, and the method has less three wastes and is more environment-friendly.
Interplay between a Foldamer Helix and a Macrocycle in a Foldarotaxane Architecture
Gauthier, Maxime,Koehler, Victor,Clavel, Caroline,Kauffmann, Brice,Huc, Ivan,Ferrand, Yann,Coutrot, Frédéric
supporting information, p. 8380 - 8384 (2021/03/16)
The design and synthesis of a novel rotaxane/foldaxane hybrid architecture is reported. The winding of an aromatic oligoamide helix host around a dumbbell-shaped thread-like guest, or axle, already surrounded by a macrocycle was evidenced by NMR spectrosc
Discovery of New Imidazo[2,1- b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising in Vitro and in Vivo Anti-melanoma Activity
Abdel-Maksoud, Mohammed S.,El-Gamal, Mohammed I.,Lee, Bong S.,Gamal El-Din, Mahmoud M.,Jeon, Hong R.,Kwon, Dow,Ammar, Usama M.,Mersal, Karim I.,Ali, Eslam M. H.,Lee, Kyung-Tae,Yoo, Kyung Ho,Han, Dong Keun,Lee, Jae Kyun,Kim, Garam,Choi, Hong Seok,Kwon, Young Jik,Lee, Kwan Hyi,Oh, Chang Hyun
, p. 6877 - 6901 (2021/06/25)
BRAF is an important component of MAPK cascade. Mutation of BRAF, in particular V600E, leads to hyperactivation of the MAPK pathway and uncontrolled cellular growth. Resistance to selective inhibitors of mutated BRAF is a major obstacle against treatment of many cancer types. In this work, a series of new (imidazo[2,1-b]thiazol-5-yl)pyrimidine derivatives possessing a terminal sulfonamide moiety were synthesized. Pan-RAF inhibitory effect of the new series was investigated, and structure-activity relationship is discussed. Antiproliferative activity of the target compounds was tested against the NCI-60 cell line panel. The most active compounds were further tested to obtain their IC50 values against cancer cells. Compound 27c with terminal open chain sulfonamide and 38a with a cyclic sulfamide moiety showed the highest activity in enzymatic and cellular assay, and both compounds were able to inhibit phosphorylation of MEK and ERK. Compound 38a was selected for testing its in vivo activity against melanoma. Cellular and animal activities are reported.
