149427-84-9Relevant articles and documents
Synthesis of functionalized pyrrolidin-2-ones and (S)-vigabatrin from pyrrole
Gheorghe, Alexandru,Schulte, Michael,Reiser, Oliver
, p. 2173 - 2176 (2006)
Starting from pyrrole, the novel 3,4-didehydropyrohomoglutamate 8 or (ent)-8 can be efficiently synthesized in up to 91% ee, which can be utilized as a versatile building block toward functionalized pyrrolidin-2-ones. Moreover, (ent)-8 can be readily converted to (S)-Vigabatrin, being an irreversible inhibitor for GABA-T, which is used as adjunctive therapy in patients that suffer from epilepsy.
NOVEL FUNCTIONALIZED LACTAMS AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE
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Paragraph 000729-000730, (2021/05/21)
Described herein are new, selective modulators of the 5 -HT7 receptor. These selective compounds can be useful for the treatment of CNS and non-CNS indications. Compounds described herein can be selective in targeting 5-HT7 receptors
NOVEL FUNCTIONALIZED LACTAMS AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE
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Paragraph 01136; 01137, (2019/11/28)
Pharmaceutical compositions of the invention comprise functionalized lactam derivatives of formula (I) having a disease-modifying action in the treatment of diseases associated with dysregulation of 5- hydroxytryptamine receptor 7 activity. A is selected
An asymmetric total synthesis of martinellic acid
Badarinarayana, Vivek,Mahmud, Hossen,Lovely, Carl J.
, p. 1082 - 1105 (2019/11/14)
We describe an asymmetric total synthesis of the pyrrolo[3,2-c]quinoline natural product martinellic acid starting from pyrroglutamic acid. A convergent strategy involving a Pd-catalyzed aryl amination reaction of a chiral, non-racemic pyrrolidine derivative incorporates the C2-chiral center which controls the remaining two stereocenters. Elaboration of this adduct through a Grieco-elimination sets the stage for a diastereoselective intramolecular [3+2] azomethine ylide-alkene cycloaddition and the construction of the remaining two chiral centers. Elaboration of the cycloadduct and incorporation the prenyl guanidine units delivered martinellic acid after removal of the protecting groups.
Total synthesis of (-)-martinellic acid
Badarinarayana, Vivek,Lovely, Carl J.
, p. 2607 - 2610 (2007/10/03)
An enantioselective formal total synthesis of the pyrrolo[3,2-c]quinoline natural product martinellic acid has been achieved. The key steps involve a Pd-catalyzed aryl amidation reaction of a pyrroglutamate derivative, an intramolecular [3+2] azomethine ylide-alkene cycloaddition and a reductive ring opening reaction.
Total synthesis of (+)-batzelladine A and (-)-batzelladine D via [4 + 2]-annulation of vinyl carbodiimides with N-alkyl imines
Arnold, Michael A.,Day, Kenneth A.,Duron, Sergio G.,Gin, David Y.
, p. 13255 - 13260 (2008/03/11)
A diastereoselective [4 + 2]-annulation of vinyl carbodiimides with chiral N-alkyl imines has been developed to access the stereochemically rich polycyclic guanidine cores of the batzelladine alkaloids. Application of this strategy, together with additional key steps such as long-range directed hydrogenation and diastereoselective intramolecular iodo-amination, led to highly convergent total syntheses of (-)-batzelladine D and (+)-batzelladine A with excellent stereocontrol.
Enantioselective Synthesis of (5R,9R)-5-Propyl-octahydroindolizine
Fleurant, Anne,Celerier, Jean Pierre,Lhommet, Gerard
, p. 695 - 696 (2007/10/02)
A versatile and practical synthesis of the dendrobatid alkaloid 167B is described using a chiral amino acid as starting material.
