121370-56-7Relevant articles and documents
1-methylpurine-4-methyleneandrostane-triazole derivative, synthesis method and application thereof
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Paragraph 0089; 0091; 0092, (2019/02/13)
The invention belongs to the technical field of medicinal chemistry, and relates to a 1- methylpurine-4- methyleneandrostane-triazole derivative with anticancer activity. The compound has the generalformula as shown in the specification. The derivative of the invention is prepared by using a 6-chloropurine compound as a raw material and through nucleophilic reaction, halogenation, azidation, cycloaddition and a Claisen-Schmidt condensation reaction. The preparation method is simple and the conditions are mild. These compounds have obvious inhibitory effects on cell lines such as gastric cancer and prostate cancer, can be used for preparing antitumor drugs, and provide a lead compound structure for further research on anticancer drugs.
Piperazinone compound containing piperidine ring and preparation method and application thereof
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Paragraph 0094; 0097-0099, (2018/09/08)
The invention discloses an piperazinone compound containing a piperidine ring and a preparation method and application thereof. The compound has a structure as shown in a general formula (I). The invention further provides a preparation method and application of the compound. The compound provided by the invention has activity of inhibiting AKT1 kinase to a certain degree and inhibiting PC-3 tumorcells from growing, thereby being used for preparing anti-tumor drugs. The formula is shown in the description.
Pd/PTABS: Catalyst for Room Temperature Amination of Heteroarenes
Murthy Bandaru, Siva Sankar,Bhilare, Shatrughn,Chrysochos, Nicolas,Gayakhe, Vijay,Trentin, Ivan,Schulzke, Carola,Kapdi, Anant R.
supporting information, p. 473 - 476 (2018/01/28)
A mild and highly efficient catalytic amination procedure for chloroheteroarenes at ambient temperature using the Pd/PTABS catalytic system is reported. The protocol is selective for the amination of chloroheteroarenes using secondary amines such as piperidine, pyrrolidine, and several others. The exceptional mildness of the developed protocol is beneficial for the synthesis of a crucial Buparlisib intermediate as well as the formal synthesis of Alogliptin in competitive yields.