The invention provides compounds of Formula (I):
1
wherein R
1
-R
4
, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.
Syntheses of Strychnan- and Aspidospermatan-Type Alkaloids. 9.<sup>1</sup> The Enantioselective Generation of Tetracyclic ABCE Intermediates by a Tandem Condensation, [3,3]-Sigmatropic Rearrangement, and Cyclization Sequence
作者:Martin E. Kuehne、Feng Xu
DOI:10.1021/jo970207j
日期:1997.11.1
tryptophan-derived benzyl 2-(benzylamino)-3-[3-[2-[(methoxycarbonyl)methyl]indolyl]]propionate gave tetracyclic hexahydro-1H-pyrrolo[2,3-d] intermediates with stereoselective placement of substituents for cyclization to pentacyclic Strychnos alkaloids. The benzyl ester moiety was readily removed by formation of a corresponding nitrile and reduction, thus providing enantioselective syntheses of the tetracyclic
Regio- and enantioselective iridium-catalysed allylic aminations and alkylations of dienyl esters
作者:Gunter Lipowsky、G�nter Helmchen
DOI:10.1039/b311502j
日期:——
Regio- and enantioselective iridium-catalysed allylic aminations and alkylations of dienyl substrates are presented; using phosphorus amidite L1 as ligand, aminations provided ee values of up to 97% and alkylations of up to 90%.
First asymmetric nucleophilic displacement reactions on chiral α-substituted aldehyde hydrazones
作者:Dieter Enders、Ralf Maaßen、Jan Runsink
DOI:10.1016/s0957-4166(98)00205-5
日期:1998.6
The first asymmetric nucleophilic substitution reaction on racemic α-substituted aldehydes using enantiomerically pure hydrazines as chiral auxiliaries is presented. The diastereoselectivity of the process is achieved by a dynamic kinetic resolution via the 1:1 epimeric mixture of the substrate hydrazones. The a2-reactivity (Umpolung) of the α-substituted hydrazones is accomplished by complexation