Journal ArticleDOI
Development of a Pilot Scale Process for the Anti-Alzheimer Drug (−)-Galanthamine Using Large-Scale Phenolic Oxidative Coupling and Crystallisation-Induced Chiral Conversion
TLDR
(−)-Galanthamine has been synthesised using an efficient nine-step procedure, which in large scale affords 12.4 (6.7−19.1)% overall yield.About:
This article is published in Organic Process Research & Development.The article was published on 1999-11-04. It has received 113 citations till now.read more
Citations
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Journal ArticleDOI
Discovery and resupply of pharmacologically active plant-derived natural products: A review.
Atanas G. Atanasov,Birgit Waltenberger,Eva-Maria Pferschy-Wenzig,Thomas Linder,Christoph Wawrosch,Pavel Uhrin,Veronika Temml,Limei Wang,Stefan Schwaiger,Elke H. Heiss,Judith M. Rollinger,Judith M. Rollinger,Daniela Schuster,Johannes M. Breuss,Valery N. Bochkov,Marko D. Mihovilovic,Brigitte Kopp,Rudolf Bauer,Verena M. Dirsch,Hermann Stuppner +19 more
TL;DR: While the intrinsic complexity of natural product-based drug discovery necessitates highly integrated interdisciplinary approaches, the reviewed scientific developments, recent technological advances, and research trends clearly indicate that natural products will be among the most important sources of new drugs in the future.
Journal ArticleDOI
Large-scale oxidations in the pharmaceutical industry.
Journal ArticleDOI
Large-Scale Carbonyl Reductions in the Pharmaceutical Industry
Javier Magano,Joshua R. Dunetz +1 more
TL;DR: The most common and reliable methods for the reduction of aldehydes, ketones, carboxylic acids, esters, amides, imides, and acid chlorides are discussed.
Journal ArticleDOI
Reductive Amination in the Synthesis of Pharmaceuticals.
Oleg I. Afanasyev,Ekaterina A. Kuchuk,Dmitry L. Usanov,Denis Chusov,Denis Chusov,Denis Chusov +5 more
TL;DR: This Review concisely compiles information on 71 medical substances that are synthesized by reductive amination according to the principle of action and a general synthetic scheme is provided for each compound.
References
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Journal ArticleDOI
153. Phenol oxidation and biosynthesis. Part V. The synthesis of galanthamine
D. H. R. Barton,G. W. Kirby +1 more
Journal ArticleDOI
Asymmetric Transformation of Either Enantiomer of Narwedine via Total Spontaneous Resolution Process, a Concise Solution to the Synthesis of (-)-Galanthamine
Wen-Chung Shieh,John A. Carlson +1 more
Journal ArticleDOI
New kilogram-synthesis of the anti-alzheimer drug (−)-galanthamine
Laszlo Czollner,Werner J. Frantsits,Bernhard Küenburg,Ursula Hedenig,Johannes Fröhlich,Ulrich Jordis +5 more
TL;DR: In this paper, a scalable synthesis of (−)-galanthamine, a drug being used for the treatment of Alzheimer's disease, was described, and the yield of the critical phenolic coupling step was optimized to 45-50%.
Journal ArticleDOI
An improved synthesis of galanthamine
TL;DR: In this paper, modifications in the total synthesis of the Amarylidaceae alkaloid of galanthamine from commercially available isovanillin and tyramine have resulted in a shortened reaction sequence, which is amenable to upscaling and in improved product yield.
Journal ArticleDOI
Reversal of central anticholinergic syndrome by galanthamine.
Anis Baraka,Sami Harik +1 more
TL;DR: Galanthamine produces effective, safe, and long-lasting reversal of the central anticholinergic syndrome in man.
Related Papers (5)
153. Phenol oxidation and biosynthesis. Part V. The synthesis of galanthamine
D. H. R. Barton,G. W. Kirby +1 more
Asymmetric Transformation of Either Enantiomer of Narwedine via Total Spontaneous Resolution Process, a Concise Solution to the Synthesis of (-)-Galanthamine
Wen-Chung Shieh,John A. Carlson +1 more