Convenient Synthesis and Structural Characterization of a Series of Methyl 4-[2-(cyclized amino)ethoxy]benzoate Esters as Key Intermediates in Synthesis of Selective Estrogen Receptor Modulators.
Journal Title: UNKNOWN - Year 2018, Vol 8, Issue 8
Abstract
Estrogen receptors, the important selective targets in management of serious aspects in women health challenging issues, guided the scope of drug discovery towards developing new entities treating osteoporosis and breast cancer. Tracing aminoethoxyphenyl pharmacophoric essential antagonistic group, abundantly present in Selective Estrogen Receptors Modulators (SERMs), directed the authors to study and explore the prospect to synthesize and exclusively characterize a series of methyl 4-[2-(cyclized amino)ethoxy] benzoate esters 9a-c rather than their reported free acids as fundamental and convenient key intermediates synthesizing potential SERMs. This paper describes synthesis and spectral characterization of these esters. The relative significant 1H-NMR shifts related to synthesized derivatives were illustrated. 13C-NMR data were particularly discussed. Moreover, molecular ion peaks and different fragmentation patterns in mass spectral analysis were demonstrated. Furthermore, retention time of different derivatives at specified conditions using gas chromatography-mass spectrometry was assigned. Purity of compounds was confirmed by elemental analysis; found data were within ± 0.4% of the theoretical valu
Authors and Affiliations
Maha Aboul Ela, Doaa AE Issa, Farah H Mansou
Keywords
Related Articles
- EP ID EP673074
- DOI -
- Views 55
- Downloads 0
In Vivo and In Vitro Anti-trypansomal Evaluation of Crude Methanolic Extracts of Crotalaria albicaulis and Cistanche phelypaea against Trypanosoma evansi
Camel trypanosomiasis is a major disease of economic importance in Ethiopian Somali Regional State, Ethiopia. Local people use the leaves of Crotalaria albicaulis and Cistanche phelypaea to treat this disease and complem...
Differential Responses of Cakile maritima at Two Development Stages to Salinity: Changes on Phenolic Metabolites and Related Enzymes and Antioxidant Activity
Though halophytes are naturally adapted to salinity, their salt-tolerance limits are greatly influenced by endogenous (that is, physiological development stages) and exogenous factors (that is, salinity). In this work, t...
Synthesis of New Derivatives of Thieno[2,3-d]pyrimidin-4(3H)-one and their Antimicrobial Activity
A series of new thieno[2,3-d]pyrimidin-4(3H)-one derivatives were synthesized. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. All the newly synthesized thieno[2,3-d]pyri...
EGFR Tyrosine Kinase Targeted In Silico Design and Synthesis of Novel Quinazoline Derivatives
Quinazolines are medicinally important as anti-convulsant, anti-cancer, anti-microbial, and anti-tubercular properties etc. They target epidermal growth factor receptors on tumor cells. This work is aimed to synthesize a...
Potential Anticancer Agents: Design, Synthesis of New Pyrido[1,2-a]benzimidazoles and Related Derivatives Linked to Alkylating Fragments
The incentive of the present work has been primarily directed towards the design and synthesis of some novel pyrido[1,2-a]benzimidazoles with specific functionalities believed to have alkylation ability. This combination...