1774-47-6Relevant articles and documents
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Senoff,C.V. et al.
, p. 3585 - 3589 (1971)
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Zoltewicz,Deady
, p. 1983,1990 (1972)
Stereoselective Cyclopropanation of (-)-Levoglucosenone Derivatives Using Sulfonium and Sulfoxonium Ylides
Ledingham, Edward T.,Merritt, Christopher J.,Sumby, Christopher J.,Taylor, Michelle K.,Greatrex, Ben W.
, p. 2652 - 2662 (2017)
The synthesis of tri- and tetrasubstituted cyclopropanes from 3-aryl-substituted levoglucosenones (LGO) has been developed. In contrast to the unstabilised ylide dimethylsulfonium methylide which gives epoxides from LGO via 1,2-addition, we have found that the soft nucleophile dimethylsulfoxonium methylide affords cyclopropanes in moderate yields from LGO and in excellent yields and stereoselectivity with 3-aryl LGO derivatives. The use of 1,1,3,3-tetramethylguanidine as base in DMSO to generate the ylide provided the best yields and shortest reaction times. Ester stabilised sulfonium ylides could also be used to generate tetrasubstituted cyclopropane derivatives. One of the products was converted into a cyclopropyl lactone via Baeyer-Villiger oxidation to demonstrate the utility of applying cyclopropanation chemistry to LGO. Georg Thieme Verlag Stuttgart.New York.
Preparation method of medetomidine and intermediate thereof
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Paragraph 0064; 0065; 0066; 0067, (2017/08/28)
The invention relates to a preparation method of 2-(2, 3-xylyl)-2-methyloxirane. The method is characterized in that the preparation process includes the following reaction shown as the specification, wherein Y is selected from Cl, Br, I, CH3SO4 or HSO4; alkali is selected from KOH, NaOH, LiOH, CsOH, K2CO3, Li2CO3, Cs2CO3, Na2CO3, EtONa, EtOK, (CH3)2CHONa, (CH3)2CHOK, (CH3)3CONa, (CH3)3COK, NH2Na or NH2K. The invention adopts the synthesis method using the 2-(2, 3-xylyl)-2-methyloxirane critical intermediate to prepare medetomidine.
1-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives, preparation methods and uses thereof
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Paragraph 0102, (2013/09/12)
Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.