- Pentazocine prodrug as well as preparation method and application thereof
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The invention discloses a pentazocine prodrug shown as a formula (I), a preparation method thereof and medical application of a pharmaceutical preparation containing the pentazocine prodrug, wherein Ris hydrogen or deuterium. The water solubility of the prodrug compound is improved by 20 times or above at room temperature, the prodrug compound is chemically stable, the onset time is delayed, thedrug effect is prolonged, meanwhile, the same parent drug blood concentration is generated at a low dosage, and the prodrug compound has a wide clinical application prospect.
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- Asymmetric syntheses of (-)-pentazocine and (-)-eptazocine through an aza-prins cyclization
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Two down more to go: The asymmetric syntheses of (-)-pentazocine and (-)-eptazocine are presented. The highlights of the syntheses are the construction of the core skeleton through an aza-Prins cyclization and intramolecular Friedel-Crafts reaction. Copyr
- Chen, Qiang,Huo, Xing,Yang, Zhen,She, Xuegong
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p. 2543 - 2546,4
(2020/09/02)
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- Enantiocontrolled synthesis of (-)-9-epi-pentazocine and (-)-aphanorphine
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(Chemical Equation Presented) We have developed novel asymmetric routes to (-)-9-epi-pentazocine and (-)-aphanorphine from a D-tyrosine derivative. The tricyclic frameworks of (-)-9-epi-pentazocine and (-)-aphanorphine were assembled stereoselectively via intramolecular Friedel-Crafts reaction of the corresponding bicyclic precursors, generated with titanium-promoted enyne cyclization and indium-initiated atom-transfer radical cyclization, respectively.
- Yang, Xiaobao,Zhai, Hongbin,Li, Zhong
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supporting information; experimental part
p. 2457 - 2460
(2009/05/26)
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- Combination of selected opioids with muscarine antagonists for treating urinary incontinence
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Active compound combinations of compounds of group A, particularly opioids, and compounds of group B, particularly anti-muscarine agents and other substances suitable for treatment of an increased urge to urinate or urinary incontinence. Related pharmaceutical formulations and methods of treatment of an increased urge to urinate or urinary incontinence are also provided.
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- Migratory hydroamination: A facile enantioselective synthesis of benzomorphans
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We describe a highly efficient, general strategy for the enantioselective synthesis of benzomorphans (45-46% overall yield from commercially available material). The new synthesis demonstrates the effectiveness of an unprecedented diastereoselective cycloisomerization via migratory hydroamination and the power of palladium-catalyzed asymmetric allylic alkylation (AAA) of simple ketone enolates in the context of complex synthesis. The strategy outlined here for the enantioselective synthesis of three contiguous stereogenic centers and the novel cycloisomerization should have many applications in alkaloid synthesis. Copyright
- Trost, Barry M.,Tang, Weiping
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p. 8744 - 8745
(2007/10/03)
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- Analgesic 3-(3-methyl-3-butenyl)-1,2,3,4,5,6-hexahydro-6,11-dimethyl-8-hydroxy-2,6-methano-3-benzazocine
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Disclosed is 3-(3-methyl-3-butenyl)-1, 2, 3, 4, 5, 6-hexahydro-6, 11-dimethyl-8-hydroxy-2, 6-methano-3-benzazocine, a new derivative of benzazocine, which has superior analgesic properties.
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