- Application of benzene in preparation 3 - bromomethyl -7 - chlorobenzene and (b) thiophene
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The invention provides an application of benzene in preparation 3 - bromomethyl -7 -chlorobenzo (b) thiophene, wherein benzene is used as a solvent in the process of preparing 3 -bromomethyl -7 -chlorobenzo (b) thiophene in 3 - methyl -7 -chlorobenzene and (b) thiophene. 3 - Bromomethyl -7 - chlorobenzene and (b) thiophene are prepared by using benzene instead of carbon tetrachloride as a solvent for bromination reaction, and the yield of the obtained product can reach above 57% and higher than that of 3 - bromomethyl -7 - chlorobenzene and (b) thiophene by using carbon tetrachloride as a solvent for bromination reaction.
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Paragraph 0042-0051
(2021/10/16)
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- Preparation process of sertaconazole nitrate
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The invention provides a preparation process of sertaconazole nitrate. The preparation process comprises the following steps: acylating, cyclizing, brominating, salifying and refining to obtain the finished product of sertaconazole nitrate. By adopting the preparation process of sertaconazole nitrate, the obtained finished product of sertaconazole nitrate is high in purity and high in yield. By adopting the preparation process of the sertaconazole nitrate, the raw materials are fully reacted, the generation of impurities is effectively reduced, the purity of a crude product is greatly improved, finally, the finished product of the sertaconazole nitrate obtained by adopting a refining process is high in purity and yield, and the production benefit of a sertaconazole nitrate bulk drug is effectively improved.
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Paragraph 0025; 0030-0031
(2021/04/26)
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- Method for synthesizing 3 - bromomethyl -7 -chlorobenzo [b] thiophene
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The invention discloses a synthesis method of 3 - bromomethyl -7 -chlorobenzo [b] thiophene. The method comprises the following steps: adding a substrate 3 - methyl -7 -chlorobenzo [b] thiophene to the linear alkane of C6 - C8 serving as a solvent, adding the initiator benzoyl peroxide under stirring, heating to boiling, adding the bromination agent N - bromosuccinimide in a batch mode, and continuing the stirring reaction under boiling. 3 - Bromomethyl -7 - chlorobenzo [b] thiophene is prepared by using C6 - C8 linear alkane as a reaction solvent through bromination reaction. C6 - C8 linear alkanes are less toxic than carbon tetrachloride. The atmospheric ozone layer is not destroyed. Moreover, the use is not limited and is more suitable for industrial production.
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Paragraph 0044-0065
(2021/10/11)
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- Synthesis and Structure-Activity Relationship of Benzothienylallylamine Antimycotics
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Benzothiophene analogues of the allylamine antimycotic terbinafine (2) bearing the side chain at various positions and optionally substituted by halogen have been prepared and their antifungal activity studied.Derivatives bearing the side chain at positions 3, 4, or 7 are bioequivalents of 2.Compounds containing the allylamine side chain at position 7, with a further substituent at position 3, showed significantly enhanced activity against Candida albicans, an effect which appears to be specifically linked only to this particular substitution pattern. 3-Chloro-7-benzothienyl derivative 7m was found to be the most potent allylamine antimycotic identified so far.In general, substituted benzothiophenes can be used not only as potential equivalents of naphthalene in bioactive compoudns but also as a tool to selectively modify biological activities.
- Nussbaumer, Peter,Petranyi, Gabor,Stuetz, Anton
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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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