- Br?nsted Acid-Catalyzed Intramolecular Hydroarylation of β-Benzylstyrenes
-
Using triphenylmethylium tetrakis(pentafluorophenyl)borate as a convenient Br?nsted acid precatalyst, β-(α,α-dimethylbenzyl)styrenes are shown to cyclize efficiently to afford a variety of new indanes that possess a benzylic quaternary center. The geminal dimethyl-containing quaternary center is proposed to be necessary to arm the substrate for cyclization through steric biasing.
- Cai, Xiao,Keshavarz, Amir,Omaque, Justin D.,Stokes, Benjamin J.
-
p. 2626 - 2629
(2017/05/24)
-
- Biarylphosphonite gold(I) complexes as superior catalysts for oxidative cyclization of propynyl arenes into indan-2-ones
-
Striking gold: A series of variously functionalized propynyl arenes was smoothly converted into indan-2-ones by a new gold(I)-catalyzed oxidative cyclization process. [LAu]NTf2 (Tf=trifluoromethanesulfonyl) is a superior catalyst both in terms of yield and kinetics for the present transformation. Copyright
- Henrion, Guilhem,Chavas, Thomas E. J.,Le Goff, Xavier,Gagosz, Fabien
-
supporting information
p. 6277 - 6282
(2013/07/11)
-
- Fe-catalyzed regiodivergent [1,2]-shift of α-aryl aldehydes
-
An Fe-catalyzed conversion of aldehydes to ketones via [1,2]-shift has been developed. This skeletal rearrangement shows a wide substrate scope and chemoselectivity profile while exhibiting an excellent [1,2]-aryl or [1,2]-alkyl shift selectivity that is easily switched by electronic effects.
- Gutierrez-Bonet, Alvaro,Flores-Gaspar, Areli,Martin, Ruben
-
supporting information
p. 12576 - 12579
(2013/09/23)
-
- Gold-catalyzed double migration-benzannulation cascade toward naphthalenes
-
(Chemical Equation Presented) A novel gold(I)-catalyzed cycloisomerization of propargylic esters leading to unsymmetrically substituted naphthalenes has been developed. This cascade reaction involves an unprecedented tandem sequence of 1,3- and 1,2-migration of two different migrating groups. It is believed that this transformation likely proceeds via the formation of 1,3-diene intermediate or its precursor, which upon cyclization and aromatization steps transforms into the naphthalene core. 2008 American Chemical Society.
- Dudnik, Alexander S.,Schwier, Todd,Gevorgyan, Vladimir
-
supporting information; experimental part
p. 1465 - 1468
(2009/04/10)
-
- Method of treating addiction or dependence using a ligand for a monoamine receptor or transporter
-
One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.
- -
-
-
- Ligands for monoamine receptors and transporters, and methods of use thereof
-
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
- -
-
-
- Nonsteroidal gestagens
-
This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2and R3have the meanings that are indicated in more detail in the description. The new compounds show a very great affin
- -
-
Page column 14-15
(2010/11/29)
-
- Therapeutic agents
-
Compounds of formula I STR1 in which R1 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, cycloalkylalkyl or optionally substituted phenyl; R2 is H or C1-3 alkyl; R3 and/or R4 are H, formyl, C1-3 alkyl, C3-6 alkenyl, C3-6 alkynyl, C3-7 cycloalkyl or R3 and R4 together with the nitrogen atom form a heterocyclic ring system; R5 and/or R6 are H, halo, CF3, C1-3 alkyl, C1-3 alkoxy, C1-3 alkylthio or R5 and R6 together with the carbon atoms to which they are attached form a second benzene ring show therapeutic activity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.
- -
-
-