Novel approaches towards the LTD4/e4 antagonist, LY290154
(2006) Organic Process Research and Development — Vol. 10, n° 4, p. 776-783 (2006)
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- Abstract
- Several novel approaches have been investigated for the synthesis of the LTD4/E-4 antagonist LY290154. Significant improvements to the discovery route were first made by using an indoline nucleophile instead of an indolyl anion in the key substitution step. An alternative approach, introducing the 7-chloroquinoline moiety in the latest stages of the synthesis was then demonstrated. Interestingly, the pivotal intermediate of this latter route was also obtained in a one-pot process following a Katritzky methodology. Finally, an asymmetric synthesis offering significant advantages over the enantioselective route reported by McKillop was demonstrated.
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Citations
Merschaert, A., Boquel, P., Van Hoeck, J.-P., Gorissen, H., Borghese, A., Bonnier, B., Mockel, A., & Napora, F. (2006). Novel approaches towards the LTD4/e4 antagonist, LY290154. Organic Process Research and Development, 10(4), 776-783. https://doi.org/10.1021/op060036x (Original work published 2006)