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Synthesis of indole oxazolines, potent 5-HT3 antagonists

✍ Scribed by Christopher J Swain; Clare Kueen; Raymond Baker

Book ID
104228643
Publisher
Elsevier Science
Year
1990
Tongue
French
Weight
225 KB
Volume
31
Category
Article
ISSN
0040-4039

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✦ Synopsis

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 axabicyclic nitrogen.

πŸ“œ SIMILAR VOLUMES

Azabicyclic indole esters as potent 5-HT
Azabicyclic indole esters as potent 5-HT4 receptor antagonists
✍ Paul A. Wyman; Laramie M. Gaster; Frank D. King; Jonathon M. Sutton; Elizabeth S πŸ“‚ Article πŸ“… 1996 πŸ› Elsevier Science 🌐 English βš– 641 KB

The synthesis of a series of azabicyclic indole esters is described and their potency reported as 5-HT4 receptor antagonists. Optimization of the most potent compound (19) by preparing the corresponding oxazino[3,2-a]indole ester afforded 34, which had a pIC50 of 9.5 in the guinea pig distal colon l