42872-30-0Relevant articles and documents
Assembly of α-(Hetero)aryl Nitriles via Copper-Catalyzed Coupling Reactions with (Hetero)aryl Chlorides and Bromides
Chen, Ying,Xu, Lanting,Jiang, Yongwen,Ma, Dawei
supporting information, p. 7082 - 7086 (2021/02/26)
α-(Hetero)aryl nitriles are important structural motifs for pharmaceutical design. The known methods for direct synthesis of these compounds via coupling with (hetero)aryl halides suffer from narrow reaction scope. Herein, we report that the combination of copper salts and oxalic diamides enables the coupling of a variety of (hetero)aryl halides (Cl, Br) and ethyl cyanoacetate under mild conditions, affording α-(hetero)arylacetonitriles via one-pot decarboxylation. Additionally, the CuBr/oxalic diamide catalyzed coupling of (hetero)aryl bromides with α-alkyl-substituted ethyl cyanoacetates proceeds smoothly at 60 °C, leading to the formation of α-alkyl (hetero)arylacetonitriles after decarboxylation. The method features a general substrate scope and is compatible with various functionalities and heteroaryls.
Application of novel dimethyl carbonate methylation catalyst in preparation α- methyl phenylacetic acid
-
Paragraph 0062-0064, (2020/03/17)
The invention relates to the field, of medicine synthesis, and concretely relates to a novel dimethyl carbonate methylation catalyst α - in preparation IV methylbenzene acetic acid. as starting material I for preparing a target product, methylbenzeneacetic acid, by a methylation, decarboxylation and hydrolysis reaction, under the action of a catalyst by using a catalyst as a representative low-cost catalyst, in the form of a quaternary amine salt, and a catalyst prepared by using the catalyst as a representative low-cost catalyst, such as potassium α - potassium bromide acetate, as a catalyst, and a catalyst used in the, hydrolysis reaction of the quaternary, amine salt. IV. 98%. The preparation method comprises the following steps: preparing a target product from the quaternary ammonium. salt solution.
Ketoprofen intermediate as well as preparation method and application thereof
-
Paragraph 0190-0192, (2019/05/02)
The invention relates to the field of medicine synthesis, in particular to a Ketoprofen intermediate as well as a preparation method and application thereof. Ketoprofen is prepared from p--nitrohalobenzene and o-nitrohalobenzene or a mixture of the p-nitrohalobenzene and the o-nitrohalobenzene as raw materials by first performing Diels-Alder reaction on the raw materials and phenylacetonitrile toobtain an isoxazole compound, and then sequentially carrying out oxidation reaction, substitution reaction, reduction reaction, deamination, ester removal and acid hydrolysis reaction to prepare the ketoprofen. The reaction formula is as shown in the specification, wherein X2 and a group as shown in the specification are located in ortho-position or para-position of a nitro group or an amino group, R1 is-CONR4R5,-COX1,-COOR2 or-CN, R2, R3, R4 and R5 are same or differently H or a C1-C6 alkyl group, and X1 and X2 are the same or different, and are F, Cl, Br Or I.
