New kilogram-synthesis of the anti-alzheimer drug (−)-galanthamine
✍ Scribed by Laszlo Czollner; Werner Frantsits; Bernhard Küenburg; Ursula Hedenig; Johannes Fröhlich; Ulrich Jordis
- Book ID
- 104259028
- Publisher
- Elsevier Science
- Year
- 1998
- Tongue
- French
- Weight
- 94 KB
- Volume
- 39
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
A concise, scalable synthesis of (-)-galanthamine, a drug being used for the treatment of Alzhcimer's disease, is described. The yield of the critical phenolic coupling step was optimized to 45-50¢7,. For the reducti~m ~I the aryl bromide, air-activated LiAIH4 was used and racemic narwedine was converted to (-)-narwedinc by a soc~)nd order asymmetric transformation.
📜 SIMILAR VOLUMES
The anti-HIV nucleotide analogue PMPA can be prepared on a kilogram-scale by a three step sequence: i) condensation of adenine with (R)-propylene carbonate, ii) alkylation of the resulting (R)-9-(2-hydroxypropyl)adenine with diethyl p-toluenesulfonyloxymethanephosphonate using lithium tert-butoxide