203661-69-2Relevant articles and documents
Synthesis of trisubstituted alkenes by Ni-catalyzed hydroalkylation of internal alkynes with cycloketone oxime esters
Lu, Xiao-Yu,Liu, Chuang-Chuang,Jiang, Run-Chuang,Yan, Lu-Yu,Liu, Qi-Le,Wang, Qing-Qing,Li, Jia-Mei
, p. 14191 - 14194 (2020/11/24)
A method for Ni-catalyzed hydroalkylation of internal alkynes with cycloketone oxime esters was developed. The reaction has a broad substrate scope. This hydroalkylation shows excellent regio-and stereo-selectivity. This method enables readily available starting materials to be used to access a range of cyano-substituted single-configuration trisubstituted alkenes. These are valuable feedstock chemicals and are widely used in synthetic and medicinal chemistry.
1-azaspirocycle compound, and preparation method and applications thereof
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, (2018/09/14)
The invention discloses a 1-azaspirocycle compound, and preparation method and applications thereof, and belongs to the field of pharmaceutical chemistry. The 1-azaspirocycle compound with a structurerepresented by formula I, or a pharmaceutically acceptable salt or a stereisomer or a solvate or a prodrug thereof is capable of realzing combination with Autotaxin, can be taken as an Autotaxin inhibitor, and can be used for prevention and treatment of diseases with Autotaxin expression increasing pathological characteristics such as cancer and fibrosis diseases especially pulmonary fibrosis andhepatic fibrosis, metabolic diseases, myelodysplastic syndrome, cardiovascular diseases, autoimmune diseases, inflammation, neurological diseasses, or pain. Compared with single component inhibitors,the 1-azaspirocycle compound and the derivatives possesses following advantages: blocking and interfacing at the upsteam of a plurality of key signal channels are realized, tumor cell growth and transfer are relieved or dalyed, early caused drug resistance is avoided, and novel means are provided for treatment of tumor cells.
Synthetic methods of 7-azaspiro[3,5]-nonane-2-ol and hydrochloride compound thereof
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Paragraph 0037-0038, (2017/07/11)
The invention discloses 7-azaspiro-[3,5]-nonane-2-ol and a hydrochloride compound thereof. Concretely, N-Boc-4-piperidone is used as a raw material, a wittig reaction is carried out in order to prepare N-Boc-4-methylenepiperidine, zinc/copper is used for catalysis of trichloroacetyl chloride in order to carry out [2+2] cyclisation for preparing N-Boc-7-azaspiro ketone; the azaspiro ketone intermediate is reduced into N-Boc-7-azaspiro-ol by sodium borohydride at a room temperature, and finally 2mol/L hydrochloric acid-ethyl acetate is used for removing Boc in order to prepare a target product hydrochloride whose purity reaches 98%. The product has the advantages of economical and easily available reagents and raw materials which are needed, simple operation, and high product purity; and the product is suitable for batch production.