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.
Ketoprofen intermediate as well as preparation method and application thereof
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Paragraph 0190-0192, (2020/03/12)
The invention relates to the field, of medicine synthesis, in particular to a ketoprofen intermediate and a preparation method and application. thereof to prepare the ketoprofen, reaction formula by sequentially performing an oxidation reaction, substitution reaction, deamination, deamination and an acidic hydrolysis reaction after formation of the isoxazole compound, by a Diels,Alder reaction with a phenylacetic acid by. a Diels :Alder reaction of a phenylacetic acid. In-flight, X2 or. Ortho or para, R to nitro or amino group1 - COCONR4 R5 , COX1 , COOR2 Or - CNCNCNR2 , R3 , R4 , R5 , R6 The same or different is H or C. 1 - C6 Alkyl, X1 , X2 The same or different is F, Cl, Br or I.
Ketoprofen intermediate as well as preparation method and application thereof
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, (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.