- Method for synthesizing 3 - halo methyl benzofuran compounds
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The invention provides a method for efficiently synthesizing a 3-halomethylation benzofuran class compound by one step through a 2-propargyloxy aniline class compound. Compared with an existing method, the method can adapt to substrates for a wide range, the compound is convenient and easy to obtain, the reaction condition is mild, the operation is easy and convenient, and the reaction efficiency is high. By means of the method, metal salt compounds do not need to be added, and the production and processing for drugs are facilitated.
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Paragraph 0068; 0069; 0094; 0095; 0096
(2019/03/21)
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- 5-Halobenzothiophene analogues of melatonin: Synthesis and affinity for mt1 and MT2 receptors in man
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A novel series of melatonin analogues based on the benzothiophene nucleus is described. In these compounds the methoxy group was replaced by electron-attracting groups such halogens (Br and Cl) with the aim of supplementing structure-affinity relationship
- Leclerc,Beaurain,Depreux,Bennejean,Delagrange,Boutin,Lesieur
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- New serotonin 5-HT1F agonists
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This invention provides novel 5-HT1Fagonists of formula where X, Y, Z,and R are defined in the specification, which are useful for the prevention and treatment of migraine and associated disorders.
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- Halogeno-Substituted 2- and 3-Methylbenzothiophenes: Use of 1H NMR Spectral Analysis and 1H Nuclear Overhauser Effect for Locating the Halogen Substituent
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Thirty-seven halogeno-substituted 2- and 3-methyl-(or halogenomethyl)-benzothiophenes, including 17 new compounds, were prepared.The constitution of 14 of these was confirmed by full analysis (LAOCOON) of their 80 MHz 1H NMR spectra and by 1H NOE measurements.In this way a by-product from the preparation of 4- and 6-bromo-3-bromomethylbenzothiophenes was shown conclusively to be 5-bromo-3-bromomethylbenzothiophene.The 3-substituted benzothiophenes showed greater NOE enhancement factors at H-4 than at H-2 when the 3-methyl or halogenomethyl substituent was irradiated.
- Cuberes, M. Rosa,Moreno-Manas, Marcial,Sanchez-Ferrando, Francisco
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p. 814 - 821
(2007/10/02)
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- Benzo[b]thiophene derivatives. XXVIII. 5-Bromo-3-benzo[b]thienylalanine and derivatives
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A potential inhibitor of gelation of sickle hemoglobin, 5-bromo-3-benzo[b]thienylalanine, has been synthesized along with several derivatives. Several hydrolytic pathways from the intermediate ethyl 5-bromo-3-benzo[b]thienylformamidomalonate have been exa
- Campaigne,Kim
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p. 1069 - 1071
(2007/10/02)
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