The synthesis of a series of indole oxaaolines is reported, proceding y& addition of an azabicyclic amino alcohol, in which the axacyclic nitrogen is borane protected, to an indole imidate. Selective alkylation of the indole nitrogen is facilitated by the bortme protection of the highly nucleophilic
β¦ LIBER β¦
Synthesis of indole oxazolines; novel 5-HT3 antagonists
β Scribed by Swain, Christopher J.; Kneen, Clare; Herbert, Richard; Baker, Raymond
- Book ID
- 120008335
- Publisher
- Royal Society of Chemistry
- Year
- 1990
- Weight
- 623 KB
- Volume
- 11
- Category
- Article
- ISSN
- 1472-7781
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## Abstract Syntheses of labelled versions of 5βHT~3~ receptor antagonists, Alosetron and Lurosetron, are described. [^14^C]Alosetron was prepared by routes utilizing either Fischer indolisation of an amidohydrazine or palladiumβmediated cyclisation of an aryl enaminone as key steps. ^2^H and ^13^C