- 5 - azaspiro [2.4] heptane - 6 - carboxylic acid derivatives of the synthesis method (by machine translation)
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The present invention provides a (5S) - 5 - azaspiro [2.4] heptane - 6 - carboxylic acid derivatives of the synthetic method, in order to 1, 1 - cyclopropane dicarboxylic alcohol as the starting material, the reaction with thionyl chloride, is oxidized and get sulfonic acid ester compound, then with glycine methyl ester imine under the action of the tertiary butyl alcohol potassium condensation, again through the system acidic, alkaline methylsulphonyl complete hydrolysis, cyclization, amino protection of the racemic product, finally split to obtain the finished product, the total yield up to 30% or more, the reaction route step is short, reagent used in the security, the operation is simple, of low cost, high yield, suitable for industrial production. (by machine translation)
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Paragraph 0045-0047
(2017/08/25)
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- Nickel-Catalyzed Asymmetric Kumada Cross-Coupling of Symmetric Cyclic Sulfates
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Nickel-catalyzed enantioselective cross-couplings between symmetric cyclic sulfates and aromatic Grignard reagents are described. These reactions are effective with a broad range of substituted cyclic sulfates and deliver products with asymmetric tertiary carbon centers. Mechanistic experiments point to a stereoinvertive SN2-like oxidative addition of a nickel complex to the electrophilic substrate.
- Eno, Meredith S.,Lu, Alexander,Morken, James P.
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supporting information
p. 7824 - 7827
(2016/07/11)
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