- HYDROXYNORKETAMINE DERIVATIVES FOR THE TREATMENT OF CNS DISORDERS
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Chemical entities of Formula (I): Including enantiomers thereof, wherein R1 has any of the values described herein, and compositions comprising such chemical entities; their preparation; and their use in various methods, including the treatment of depression, pain, cognitive disorders, neurodegenerative disorders, and other neurological and peripheral disorders.
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- COMPOUNDS FOR THERAPEUTIC USE
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Chemical entities of Formula (I): Including enantiomers thereof, wherein R1 has any of the values described herein, and compositions comprising such chemical entities; their preparation; and their use in various methods, including the treatment of depression, pain, cognitive disorders, neurodegenerative disorders, and other neurological and peripheral disorders.
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- Synthesis of Ketamine Metabolites I and II and Some Anomalous Reactions of 6-Bromoketamine
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Two metabolites of the drug ketamine, 2-(2-chlorophenyl)-2-(methylamino)cyclohexanone hydrochloride (1), have been synthesized.They are the N-demethyl compound, metabolite I (13), and the N-demethyl-5,6-dehydro analogue, metabolite II (15).Three bromo ketone derived from ketamine have also been synthesized and their realtive configuration assigned.In addition, attempted dehydrohalogenation of axial 2-bromoketamine (2a) with sodium amide in liquid ammonia has produced a novel entry into the 6-azabicycloheptane ring system.The structure of the rearrangement product (3) has been confirmed by unequivocal synthesis.Other unusual reactions include the reduction of an N-alkylazetidinone to an N-alkylazetidine and an acid-catalyzed N-alkyl cleavage of a β-lactam.
- Parcell, Robert F.,Sanchez, Joseph P.
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p. 5055 - 5060
(2007/10/02)
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