89638-21-1Relevant articles and documents
Stereodivergent Desymmetrization of Simple Dicarboxylates via Branch-Selective Pd/Cu Catalyzed Allylic Substitution
Huo, Xiaohong,Li, Guanlin,Luo, Yicong,Peng, Youbin,Xu, Kai,Zhang, Wanbin,Zhao, Ling
supporting information, (2022/04/03)
Asymmetric desymmetrization has been demonstrated to be a powerful strategy for building stereocenters in asymmetric synthesis. Herein, a Pd/Cu catalyzed asymmetric desymmetrization reaction with a simple geminal dicarboxylate is reported. A wide scope of imino esters bearing an aryl or heteroaromatic group were compatible with this bimetallic catalytic system. The reactions proceeded smoothly, giving the desired products in good yields with high to excellent regio-, diastereo-, and enantioselectivity (up to 20 : 1 branched:linear, >20 : 1 dr, >99 % ee). Notably, the reaction favored branched selectivity, which is unusual for the Pd-catalyzed allylic alkylation reaction. In addition, the standard product could be easily transformed to other valuable molecules such as chiral allylic alcohols, carbamates, and organic boron compounds. Furthermore, DFT calculations were conducted to explain the origin of the branched selectivity.
Novel synthetic method for 7-halogen-1-indanone
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Paragraph 0035; 0036; 0037; 0038, (2018/07/07)
The invention discloses a novel synthetic method for 7-halogen-1-indanone. The reaction general formula of the method is shown in the description, wherein X is fluorine, chlorine or bromine. The method provided by the invention uses o-halogenated acetophenone as a starting raw material, an iron-catalyzed carbonyl methylenation reaction is performed to obtain a vinyl ketone, and acid-catalyzed ringclosure is performed to obtain the 7-halogen-1-indanone. The method provided by the invention has the advantages that the raw materials are simple and easy to obtain, the post-treatment is simple andthe total yield is high, and can provide an important reference for industrialized production.
CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
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Page/Page column 51; 52, (2011/01/05)
This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, Io1, Io2, Io5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
1-Alkyl-2,3-dihydro-4(1H)-quinolinones by a tandem Michael-SNAr annulation reaction
Bunce, Richard A.,Nago, Takahiro
experimental part, p. 623 - 628 (2009/11/30)
(Chemical Equation Presented) A tandem Michael-SNAr annulation reaction has been developed for the synthesis of 1-alkyl-2,3-dihydro-4(1H)- quinolinones. Success in the reaction followed expected electronic effects for the final SNAr