- Copper-Catalyzed Cascade Cyclization of Indolyl Homopropargyl Amides: Stereospecific Construction of Bridged Aza-[n.2.1] Skeletons
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Catalytic cycloisomerization-initiated cascade cyclizations of terminal alkynes have received tremendous interest, and been widely used in the facile synthesis of a diverse array of valuable complex heterocycles. However, these tandem reactions have been mostly limited to noble-metal catalysis, and are initiated by an exo-cyclization pathway. Reported herein is an unprecedented copper-catalyzed endo-cyclization-initiated tandem reaction of indolyl homopropargyl amides, where copper catalyzes both the hydroamination and Friedel–Crafts alkylation process. This method allows the practical and atom-economical synthesis of valuable bridged aza-[n.2.1] skeletons (n=3–6) with wide substrate scope, and excellent diastereoselectivity and enantioselectivity by a chirality-transfer strategy. Moreover, the mechanistic rationale for this novel cascade cyclization is also strongly supported by control experiments, and is distinctively different from the related gold catalysis.
- Tan, Tong-De,Zhu, Xin-Qi,Bu, Hao-Zhen,Deng, Guocheng,Chen, Yang-Bo,Liu, Rai-Shung,Ye, Long-Wu
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supporting information
p. 9632 - 9639
(2019/06/27)
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- Methods of treating soft tissue defects
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The specification discloses compositions and methods for treating a soft tissue defect of an individual.
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Page/Page column 68
(2016/06/01)
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- COMPOSITIONS AND IMPROVED SOFT TISSUE REPLACEMENT METHODS
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The present specification discloses compositions and methods of transplanting tissue useful for treating a soft tissue condition of an individual.
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- 2,3,4-Substituted cyclopentanones as therapeutic agents
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Disclosed herein are compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein a dashed line represents the presence or absence of a bond; Y is a carboxylic acid, sulfonic acid, or phosphonic acid functional group; or an amide or ester thereof comprising from 0 to 12 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising from 0 to 12 carbon atoms; or Y is a tetrazolyl functional group; A is —(CH2)6—, cis —CH2—CH═CH—(CH2)3—, or —CH2—C≡C—(CH2)3— wherein 1 or 2 carbons may be substituted with S or O; B is hydrogen, C1-6 hydrocarbyl, CN, CO2H, or —(CH2)mX(CH2)pH, wherein m is at least 1 and the sum of m and p is from 1 to 5; X is S or O; J is H, CH3, or CF3; D is a covalent bond, CH2, O, or S; and E is an aromatic heterobicyclic ring system which may have substituents comprising up to 6 non-hydrogen atoms each. Methods, compositions, and medicaments related thereto are also disclosed.
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Page/Page column 18; sheet 5
(2010/11/30)
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- Sleep inducing compounds and methods relating thereto
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Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
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Page/Page column 16
(2010/02/15)
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- Triflic anhydride-promoted cyclization of sulfides: A convenient synthesis of fused sulfur heterocycles
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A new approach to the synthesis of annulated sulfur heterocycles based on triflic anhydride-promoted cyclization of the hetaryl(aryl) containing alkyl sulfides was elaborated. Smooth demethylation of initially formed cyclic sulfonium salts by treatment with triethylamine afforded a number of five-, six- and seven-membered fused sulfur heterocycles. Unexpected ring opening took place in the reaction of diethylamine with 5-membered sulfonium salts.
- Shevchenko, Nikolay E.,Nenajdenko, Valentine G.,Balenkova, Elizabeth S.
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p. 1191 - 1200
(2007/10/03)
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- New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central α2-antagonistic activity as potential antidepressants
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The synthesis and biological activity of a series of benzofuro[3,2- c]pyridines and a benzothieno[3,2-c]pyridine are described. These compounds exhibit high affinity for the α2-adrenoceptor, with high selectivity versus the α1-receptor. Compound 1 also shows potent in vivo central activity and has been selected for further biological and clinical evaluation.
- Kennis, Ludo E.J.,Bischoff, Francois P.,Mertens, Carolus J.,Love, Christopher J.,Van den Keybus, Frans A.F.,Pieters, Serge,Braeken, Mirielle,Megens, Anton A.H.P.,Leysen, Josee E.
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