Journal ArticleDOI
Synthesis of (-)-morphine.
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The preparation of the diastereomerically pure beta-tetralone ketal 4 is reported and the key step in this synthesis was the bis-intramolecular cyclization of keto aldehyde 2 to give the tetracyclic intermediate 20.Abstract:
The preparation of the diastereomerically pure beta-tetralone ketal 4 is reported. Intramolecular alkylidene C-H insertion followed by hydrolysis of 4 proceeded to give the enantiomerically pure cyclopentene 15. The key step in this synthesis was the bis-intramolecular cyclization of keto aldehyde 2 to give the tetracyclic intermediate 20. Enone 20 was converted over several steps to (-)-morphine 1.read more
Citations
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C-H bond functionalization: emerging synthetic tools for natural products and pharmaceuticals
TL;DR: This Review provides an overview of C-H bond functionalization strategies for the rapid synthesis of biologically active compounds such as natural products and pharmaceutical targets.
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Funktionalisierung von C‐H‐Bindungen: neue Synthesemethoden für Naturstoffe und Pharmazeutika
TL;DR: In this paper, aufsatz gibt einen Uberblick uber die Strategien, die durch Funktionalisierung von C-H-Bindungen eine rasche Synthese von biologisch aktiven Verbindungen wie Naturstoffen und pharmazeutischen Zielsubstanzen ermoglichen.
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Mu Opioids and Their Receptors: Evolution of a Concept
TL;DR: Understanding of these morphine-like agents and their receptors has undergone an evolution in thinking over the past 35 years, which now reveals a complexity of the morphine- like agents andtheir receptors that had not been previously appreciated.
Journal ArticleDOI
Microbial production of plant benzylisoquinoline alkaloids
Hiromichi Minami,Ju-Sung Kim,Nobuhiro Ikezawa,Tomoya Takemura,Takane Katayama,Hidehiko Kumagai,Fumihiko Sato +6 more
TL;DR: The synthesis of (S)-reticuline from dopamine by crude enzymes from transgenic Escherichia coli indicates that microbial systems that incorporate plant genes cannot only enable the mass production of scarce benzylisoquinoline alkaloid alkaloids but may also open up pathways for the production of novel benzylcolysis of tyrosine.
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Natural Products as a Foundation for Drug Discovery
TL;DR: The aim of this unit is to review current strategies and techniques that increase the value of natural products as a source for novel drug candidates.
References
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Quaternary ammonium tetrakis(diperoxotungsto)phosphates(3-) as a new class of catalysts for efficient alkene epoxidation with hydrogen peroxide
Carlo Venturello,Rino D'Aloisio +1 more
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Opioids in chronic pain
TL;DR: The advance in the understanding of the biogenesis of various endogenous opioid peptides, their anatomical distribution, and the characteristics of the multiple receptors with which they interact open a new avenue for understanding the role of opioid peptide systems in chronic pain.
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Asymmetric synthesis of either enantiomer of opium alkaloids and morphinans. Total synthesis of (-)- and (+)-dihydrocodeinone and (-)- and (+)-morphine
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Synthesis and pharmacology of some 2-aminotetralins. Dopamine receptor agonists.
TL;DR: Data support the idea that the extended conformation for the phenylethylamine moiety of ampmorphine and dopamine is favorable for dopaminergic agonist activity and suggest that an unetherified catechol group may not be essential for such activity.