17514-68-0Relevant academic research and scientific papers
Chiral Benzothiophene Synthesis via Enantiospecific Coupling of Benzothiophene S-Oxides with Boronic Esters
Aggarwal, Varinder K.,Noble, Adam,Sang, Ruocheng
supporting information, p. 25313 - 25317 (2021/11/09)
Benzothiophenes are valuable heterocycles that are widely used in medicines, agrochemicals, and materials science. Herein, we report a general method for the synthesis of enantioenriched 2,3-disubstituted benzothiophenes via a transition-metal-free C2-alkylation of benzothiophenes with boronic esters. The reactions utilize benzothiophene S-oxides in lithiation-borylations to generate intermediate arylboronate complexes, and subsequent Tf2O-promoted S?O bond cleavage to trigger a Pummerer-type 1,2-metalate shift, which gives the coupled products with complete enantiospecificity. Primary, secondary and tertiary alkyl boronic esters and aryl boronic esters are successfully coupled with a range of C3-substituted benzothiophenes. Importantly, this transformation does not require the use of C3 directing groups, therefore it overcomes a major limitation of previously developed transition-metal-mediated C2 alkylations of benzothiophenes.
Preparation process of sertaconazole nitrate
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, (2021/04/26)
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.
NEW COMPOUNDS
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, (2012/04/04)
A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
BISARYLSULFONAMIDES USEFUL AS KINASE INHIBITORS IN THE TREATMENT OF INFLAMMATION AND CANCER
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, (2012/01/13)
A compound of formula (I). The compound is useful for treating cancer and inflammatory diseases. A pharmaceutical composition containing the compound.
Benzofuranyl carbamates
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, (2008/06/13)
Compounds of the structure; STR1 and pharmaceutically acceptable salts thereof, wherein: R1 is H, alkyl, alkoxy, carboxyl, alkylcarboxy, trifluoromethyl, halogen, nitro or hydroxy; X is O, N, S or C; Y is O, N or S; and R2 is H, alkyl, cycloalkyl, aryl or heteroaryl useful in the treatment of ischemic heart disease and hypertriglyceridemia.
Halogeno-Substituted 2- and 3-Methylbenzothiophenes: Use of 1H NMR Spectral Analysis and 1H Nuclear Overhauser Effect for Locating the Halogen Substituent
Cuberes, M. Rosa,Moreno-Manas, Marcial,Sanchez-Ferrando, Francisco
, p. 814 - 821 (2007/10/02)
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.
