1428932-17-5Relevant articles and documents
Preparation method of pyrrole compound
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, (2022/03/27)
The invention relates to the field of medicinal chemistry, in particular to a preparation method of a pyrrole compound. The method comprises the following steps: reacting raw materials with propionitrile in the presence of a phase transfer catalyst and an alkali reagent, and then carrying out a ring closing reaction, a substitution reaction, a sulfonylation reaction and a condensation reaction to obtain a target compound. The method is relatively short in route, simple, convenient and easy to implement, and can be used for industrial production.
Vonoprazan fumarate preparation method
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Paragraph 0023; 0032; 0040-0048, (2017/02/24)
The invention concretely relates to a vonoprazan fumarate preparation method, and belongs to the field of medicines and chemical engineering. The method comprises the following steps: 1, carrying out condensation on 2-fluoroacetophenone used as an initial raw material and allylamine to obtain a compound IV; 2, carrying out a ring closing reaction on the compound IV under the catalysis of a copper catalyst in the presence of a ligand in order to obtain a compound V; 3, carrying out a sulfoamidation reaction on the compound V and pyridine-3-sulfonyl chloride to generate a compound VII; 4, carrying out a bromination reaction on the compound VII by using N-bromosuccimide in order to generate a compound VIII; 5, carrying out an amination reaction on the compound VIII and methylamine hydrochloride under the action of a catalyst and an alkali in order to obtain vonoprazan alkali; and 6, carrying out salt formation on the vonoprazan alkali and fumaric acid in order to obtain vonoprazan fumarate. The preparation method has the advantages of simplicity in operation, mild reaction conditions, high yield and high purity of the product, and easiness in industrial production.
α-Palladation of imines as entry to dehydrogenative heck reaction: Aerobic oxidative cyclization of N-allylimines to pyrroles
Chen, Zhiyuan,Lu, Beili,Ding, Zhenhua,Gao, Ke,Yoshikai, Naohiko
supporting information, p. 1966 - 1969 (2013/06/04)
We report here a palladium(II)-catalyzed oxidative cyclization reaction of N-allylimines derived from methyl ketones, typically acetophenones, affording pyrrole derivatives at room temperature under oxygen atmosphere. The reaction likely proceeds through α-palladation of the imine followed by olefin migratory insertion and β-hydride elimination, thus representing a new example of aerobic dehydrogenative Heck cyclization.