1368802-30-5Relevant academic research and scientific papers
Preparation method of niraparib intermediate 4-(3S-piperidine-3-yl)bromobenzene
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Paragraph 0029; 0030; 0031; 0032; 0039; 0040, (2017/08/28)
The invention discloses a preparation method of niraparib intermediate 4-(3S-piperidine-3-yl)bromobenzene. The preparation method is characterized by comprising steps as follows: 1) a compound shown in a formula I and hydroxylammonium chloride are subjected to a contact reaction to produce a compound shown in a formula II; 2) the compound shown in the formula II and phenyl dichlorophosphate are subjected to a catalytic reaction to produce a compound shown in a formula III; 3) the compound shown in the formula III is subjected to a reduction reaction to produce niraparib intermediate 4-(3S-piperidine-3-yl)bromobenzene shown in a formula X, and the specific reaction process is shown in the specification. A new synthesis way is provided for the niraparib intermediate 4-(3S-piperidine-3-yl)bromobenzene, metal catalysts, expensive transaminase and the like are not used in the reaction process, the production cost is low, and the product has the good yield and stereoselectivity.
Catalytic and regioselective ring expansion of arylcyclobutanones with trimethylsilyldiazomethane. Ligand-dependent entry to β-ketosilane or enolsilane adducts
Dabrowski, Jennifer A.,Moebius, David C.,Wommack, Andrew J.,Kornahrens, Anne F.,Kingsbury, Jason S.
supporting information; experimental part, p. 3598 - 3601 (2010/11/04)
Divergent reactivity is uncovered in the homologation of arylcyclobutanones with trimethylsilyldiazomethane. With Sc(OTf)3 as catalyst, enolsilanes are obtained with a high preference for methylene migration. By contrast, Sc(hfac)3 g
