- Dianionic Phase-Transfer Catalyst for Asymmetric Fluoro-cyclization
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Inspired by the dicationic nature of the electrophilic fluorinating reagent, Selectfluor (1), we rationally designed a series of dicarboxylic acid precatalysts (2), which, when deprotonated, act as anionic phase-transfer catalysts for asymmetric fluorination of alkenes. Among them, 2a having the shortest linker moiety efficiently catalyzed unprecedented 6-endo-fluoro-cyclization of various allylic amides, affording fluorinated dihydrooxazine compounds with high enantioselectivity (up to 99% ee). In addition to cyclic substrates, acyclic trisubstituted alkenes underwent the reaction with good diastereoselectivity, whereas low diastereoselectivity was observed for linear disubstituted alkenes. Results suggest that the reaction proceeds via a fluoro-carbocation intermediate.
- Egami, Hiromichi,Niwa, Tomoki,Sato, Hitomi,Hotta, Ryo,Rouno, Daiki,Kawato, Yuji,Hamashima, Yoshitaka
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supporting information
p. 2785 - 2788
(2018/03/08)
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- Synthesis of robalzotan, ebalzotan, and rotigotine precursors via the stereoselective multienzymatic cascade reduction of α,β-unsaturated aldehydes
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A stereoselective synthesis of bicyclic primary or secondary amines, based on tetralin or chroman structural moieties, is reported. These amines are precursors of important active pharmaceutical ingredients such as rotigotine (Neupro), robalzotan, and eba
- Brenna, Elisabetta,Gatti, Francesco G.,Malpezzi, Luciana,Monti, Daniela,Parmeggiani, Fabio,Sacchetti, Alessandro
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p. 4811 - 4822
(2013/07/05)
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- TREATMENT OR PROPHYLAXIS OF PROLIFERATIVE CONDITIONS
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The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
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Page/Page column 76
(2010/11/17)
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- MONOAMINE RE-UPTAKE INHIBITORS AND METHODS RELATING THERETO
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Monoamine re-uptake inhibitors and more specifically serotonin and noradrenaline re-uptake inhibitors are disclosed that have utility in the treatment of disorders of the central or peripheral nervous system in both men and women. The compounds of this invention have the structure: wherein R1, R2, R3, R4, R5, R6, m, n, W, X, Y, and Z are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts, esters and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting monoamine re-uptake in a subject in need thereof.
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Page/Page column 26
(2010/11/25)
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- Pharmacomodulation d'adrenolytiques α en serie benzopyrannique
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Pharmacomodulation of α-adrenergic blocking agents by a series of benzopyrans.The N-methylpiperidine fragment was associated with four oxygenated heterocycles of the benzopyran ring system.Two different synthesis pathways were used in each case.Twenty intermediate derivatives and four aminomethylated derivatives whose structures were established by spectroscopic data are described.The pharmacological investigation demonstrates the interest of these compounds on the α-adrenergic receptors in light of their activities and selectivities. α1-adrenergic blocking agents / α2-adrenergic blocking agents / piperidinomethyl chromone, chromene and chromane
- Mouysset, Genevieve,Payard, Marc,Grassy, Gerard,Tronche, Pierre,Dabire, Hubert,et al.
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p. 539 - 544
(2007/10/02)
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