- 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 0040-0042
(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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- SPIROPYRROLIDINES AS MDM2 INHIBITORS
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Described are spiropyrrolidines (I) useful as inhibitors of MDM2/p53 interactions and provides useful agents for the treatment of diseases like cancer and retinal macular degeneration diseases. The invented compounds herein have the general Further described are pharmaceutical compositions that comprise one or more compounds of the invention, a pharmaceutically acceptable salt or pro-drug and/or a pharmaceutically acceptable carrier or excipient.
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Paragraph 0235-0236
(2015/11/30)
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- PREPARATION OF MONTELUKAST AND ITS SALTS
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There is provided a process for the preparation of montelukast of the Formula (I).
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Page/Page column 35-36
(2008/12/05)
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- Preparation of cyclic sulfites by transesterification of diols and diisopropyl sulfite
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Cyclic sulfites of 1,2-, 1,3- and 1,4-diols can be prepared in high yield by acid or base catalyzed transesterification with diisopropyl sulfite.
- King, Steven A.,Pipik, Brenda,Conlon, David A.,Bhupathy
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p. 701 - 707
(2007/10/03)
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- The Chemistry of 1,3-Glycol Derivatives. III. The Preparation of 1,1-Bis(1-hydroxyalkyl)cyclopropanes and Their Halogenation
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By the reduction of 1,1-diacylcyclopropanes and their related compounds, several kinds of 1,1-bis(1-hydroxyalkyl)cyclopropanes have been prepared.Some of the stereoisomers were separated, and their configurations were determined by the NMR study of the 1,3-dioxanes prepared by the acetallization of the diols.The diols were subjected to halogenation.Although the reactions of meso- and dl-bis(1-hydroxyethyl)cyclopropanes with thionyl chloride and phosphorus pentachloride gave normal dichlorides, accompanied by slight skeletal rearrangements, the stereospecificities were rather low.With ZnCl2-HCl, the specificities were lost completely and large amounts of the homoallyl derivative were formed.The reaction mechanism is discussed.
- Itoh, Osamu,Kohmura, Yoshiro,Ichikawa, Yasunori,Umezu, Makoto,Okita, Tsutomu,Ichikawa, Katsuhiko
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p. 146 - 153
(2007/10/02)
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