5118-13-8Relevant articles and documents
Base-catalyzed aryl halide isomerization enables the 4-selective substitution of 3-bromopyridines
Bandar, Jeffrey S.,Puleo, Thomas R.
, p. 10517 - 10522 (2020/10/18)
The base-catalyzed isomerization of simple aryl halides is presented and utilized to achieve the 4-selective etherification, hydroxylation and amination of 3-bromopyridines. Mechanistic studies support isomerization of 3-bromopyridines to 4-bromopyridines proceedsviapyridyne intermediates and that 4-substitution selectivity is driven by a facile aromatic substitution reaction. Useful features of a tandem aryl halide isomerization/selective interception approach to aromatic functionalization are demonstrated. Example benefits include the use of readily available and stable 3-bromopyridines in place of less available and stable 4-halogenated congeners and the ability to converge mixtures of 3- and 5-bromopyridines to a single 4-substituted product.
Synthesis method of brexpiprazole intermediate 4-bromobenzo[b]thiophene
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Paragraph 0016-0021, (2020/04/22)
The invention belongs to the field of chemical pharmacy, and particularly discloses a synthesis method of a brexpiprazole intermediate 4-bromobenzo[b]thiophene. The synthesis method comprises: carrying out a cyclization reaction with mercaptoacetic acid by using 2-bromo-6-fluorobenzaldehyde as a raw material, and carrying out a deacidification reaction to obtain the 4-bromobenzo[b]thiophene. According to the invention, triethylene diamine is used as a decarboxylation catalyst, and replaces an oxine-copper system, so that the reaction temperature is low, impurities are few, and the product yield is high; and the triethylene diamine can be recycled, so that the production cost is reduced, the generation of three wastes is reduced, and the method is environment-friendly.
HETEROCYCLIC COMPOUNDS, PROCESS FOR PREPARATION OF THE SAME AND USE THEREOF
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, (2017/07/15)
The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.