Development of an Efficient and Stereoselective Manufacturing Route to Idoxifene
…, DC Lathbury, DO Morgan, N O'Connor…
Index: Ace, Karl W.; Armitage, Mark A.; Bellingham, Richard K.; Blackler, Paul D.; Ennis, David S.; Hussain, Nigel; Lathbury, David C.; Morgan, David O.; O'Connor, Noah; Oakes, Graham H.; Passey, Stephen C.; Powling, Laurence C. Organic Process Research and Development, 2001 , vol. 5, # 5 p. 479 - 490
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Citation Number: 9
Abstract
A literature route to 1-(2-{4-[(E)-1-(4-iodophenyl)-2-phenyl-but-1-enyl] phenoxy} ethyl) pyrrolidine (idoxifene) has been modified to tackle various scale-up issues and provide initial supplies. A new highly efficient, robust, and stereoselective manufacturing route is described in detail. This route involves diastereoselective synthesis of tertiary alcohol (1 RS, 2 SR)-1-(4-iodophenyl)-2-phenyl-1-[4-(2-pyrrolidin-1-yl-ethoxy) phenyl] butan-1-ol by ...
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