An efficient asymmetric synthesis of the enantiomers of 2- aminomethyl-4-(4-fluorobenzyl)morpholine (3) which has served as an intermediate of mosapride (1), a potential gastroprokinetic agent, was achieved by the conversion of enantiomeric 3-chloro-1-(4-fluorobenzylamino)-2-propanol (8) to the oxomorpholine (10) followed by reduction and amination, in approximately 35% overall yield with > 98% ee. This synthetic route comprises the regioselective opening of homochiral epichlorohydrin (4) with 4- fluorobenzylamine, with retention of the configuration

This efficient asymmetric synthesis of 2-aminomethyl-4-(4-fluorobenzyl)morpholine, an intermediate in mosapride, was achieved by converting enantiomeric 3-chloro-1-(4-fluorobenzylamino)-2-propan

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Asymmetric synthesis of the enantiomers of 2-aminomethyl-4-(4-fluorobenzyl)morpholine, an intermediate of mosapride, a gastroprokinetic agent

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