Site-selective acylation of α-hydroxyl groups in amides has been achieved in the presence of other primary hydroxyl groups with intrinsic high reactivity. In this methodology, a relatively stable pyridine aldoxime ester was exploited as an acyl donor to suppress undesired acylation. The catalytic activation of a pyridine aldoxime ester with a Lewis acid produced a cationic complex, which preferentially
[EN] NOVEL COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS UTILISÉS COMME INHIBITEURS DE L'INDOLÉAMINE 2,3-DIOXYGÉNASE
申请人:MERCK SHARP & DOHME
公开号:WO2017106062A1
公开(公告)日:2017-06-22
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme:(I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
On the basis of the structural similarity of N-substituted glycolamides with N-glycolyl muramic acid residues of the cell wall of Mycobacterium tuberculosis, a series of these compounds were designed and synthesized by the reaction of glycolic acid acetonide 1 (2,2-dimethyl-5-oxo-1,3-dioxolane) with the proper amines. The minimum inhibitory concentration (MIC) was determined against M. tuberculosis H(37)Rv in BACTEC 12B medium, using the Microplate Alamar Blue Assay (MABA). Among the synthesized compounds, all those with disubstituted amide structure accompanied by one or two heteroatom(s) with loan pair(s) of electrons atom(s) P to the amide nitrogen demonstrated moderate anti-tuberculosis activity and all the monosubstituted amides showed no activity at all. (C) 2008 Elsevier Masson SAS. All rights reserved.
2-OXO-2-({2-[(phenylcarbamoyl)oxy]ethyl} amino)ethyl phenylcarbamate as an eco-friendly insecticidal agent against spodoptera littoralis (boisd.)
申请人:KING FAISAL UNIVERSITY
公开号:US12035717B1
公开(公告)日:2024-07-16
Synthesis of a compound 2-oxo-2-(2-[(phenylcarbamoyl)oxy]ethyl}amino)ethyl phenylcarbamate and its use as an insecticidal agent.