30962-69-7Relevant academic research and scientific papers
Copper-Catalyzed Cascade Cyclization of Indolyl Homopropargyl Amides: Stereospecific Construction of Bridged Aza-[n.2.1] Skeletons
Tan, Tong-De,Zhu, Xin-Qi,Bu, Hao-Zhen,Deng, Guocheng,Chen, Yang-Bo,Liu, Rai-Shung,Ye, Long-Wu
supporting information, p. 9632 - 9639 (2019/06/27)
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.
Methods of treating soft tissue defects
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Page/Page column 68, (2016/06/01)
The specification discloses compositions and methods for treating a soft tissue defect of an individual.
COMPOSITIONS AND IMPROVED SOFT TISSUE REPLACEMENT METHODS
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, (2012/03/10)
The present specification discloses compositions and methods of transplanting tissue useful for treating a soft tissue condition of an individual.
2,3,4-Substituted cyclopentanones as therapeutic agents
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Page/Page column 18; sheet 5, (2010/11/30)
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.
Sleep inducing compounds and methods relating thereto
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Page/Page column 16, (2010/02/15)
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.
Triflic anhydride-promoted cyclization of sulfides: A convenient synthesis of fused sulfur heterocycles
Shevchenko, Nikolay E.,Nenajdenko, Valentine G.,Balenkova, Elizabeth S.
, p. 1191 - 1200 (2007/10/03)
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.
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central α2-antagonistic activity as potential antidepressants
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.
, p. 71 - 74 (2007/10/03)
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.
