文摘
Several novel approaches have been investigated for thesynthesis of the LTD4/E4 antagonist LY290154. Significantimprovements to the discovery route were first made by usingan indoline nucleophile instead of an indolyl anion in the keysubstitution step. An alternative approach, introducing the7-chloroquinoline moiety in the latest stages of the synthesiswas then demonstrated. Interestingly, the pivotal intermediateof this latter route was also obtained in a one-pot processfollowing a Katritzky methodology. Finally, an asymmetricsynthesis offering significant advantages over the enantioselective route reported by McKillop was demonstrated.