Electric Literature of C10H8FNO2On May 31, 1988, Fagan, Gay P.; Chapleo, Christopher B.; Lane, Anthony C.; Myers, Malcolm; Roach, Alan G.; Smith, Colin F. C.; Stillings, Michael R.; Welbourn, Anthony P. published an article in Journal of Medicinal Chemistry. The article was 《Indoline analogs of idazoxan: potent α2-antagonists and α1-agonists》. The article mentions the following:
The synthesis and α-adrenergic activity of a series of substituted 2-imidazolinylindolines are described. Substitution in the indoline ring generated compounds with a spectrum of adrenoreceptor antagonist/agonist profiles that proved sensitive to both the nature and position of the substituent. Many of the derivatives possess greater presynaptic antagonist potency than the corresponding benzodioxan, dihydrobenzofuran, and indan analogs; however, this α2-antagonism is often accompanied by α1-agonist activity. It was not possible to sep. α2-antagonist from α1-agonist properties in this series. Compounds of most interest proved to be the N-Et, 5-chloro-N-Me, and 5-chloro-N-Et derivatives, all being potent α2-antagonists and α1-agonists. Substitution at the 4- and 7-position of the indoline ring generally gave compounds with nonselective agonist properties. In the part of experimental materials, we found many familiar compounds, such as Methyl 4-fluoro-1H-indole-2-carboxylate(cas: 113162-36-0Electric Literature of C10H8FNO2)
Methyl 4-fluoro-1H-indole-2-carboxylate(cas: 113162-36-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).Electric Literature of C10H8FNO2
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles