15504-60-6Relevant articles and documents
A preparation method for rosacea acetate hydrochloride
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Paragraph 0105-0106, (2021/12/07)
The present invention relates to the field of pharmaceutical preparation technology, in particular to a method for preparing rosatidine acetate hydrochloride. The present invention adopts m-hydroxybenzoic acid as a starting material, a wide range of sources, inexpensive, and it can be prepared by oxidation of m-hydroxytoluene, without involving a toxicity warning structure and nitrosamine impurities; at the same time, in this preparation process only involves a genotoxic warning structure substance, reducing the risk of medication of subsequent drugs.
Enantioselective synthesis of atropisomeric benzamides through peptide-catalyzed bromination
Barrett, Kimberly T.,Miller, Scott J.
supporting information, p. 2963 - 2966 (2013/04/10)
We report the enantioselective synthesis of atropisomeric benzamides employing catalytic electrophilic aromatic substitution reactions involving bromination. The catalyst is a simple tetrapeptide bearing a tertiary amine that may function as a Br?nsted base. A series of tri- and dibrominations were accomplished for a range of compounds bearing differential substitution patterns. Tertiary benzamides represent appropriate substrates for the reaction since they exhibit sufficiently high barriers to racemization after ortho functionalization. Mechanism-driven experiments provided some insight into the basis for selectivity. Examination of the observed products at low conversion suggested that the initial catalytic bromination may be regioselective and stereochemistry-determining. A complex between the catalyst and substrate was observed by NMR spectroscopy, revealing a specific association. Finally, the products of these reactions may be subjected to regioselective metal-halogen exchange and trapping with I2, setting the stage for utility.
