Use of DOE for rapid development of a Red-Al reduction process for the synthesis of 3, 4-isopropylidenedioxypyrrolidine hydrotosylate

AR Alimardanov, MT Barrila, FR Busch…

Index: Alimardanov, Asaf R.; Barrila, Mark T.; Busch, Frank R.; Carey, James J.; Couturier, Michel A.; Cui, Curtis Organic Process Research and Development, 2004 ,  vol. 8,  # 6  p. 834 - 837

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Citation Number: 15

Abstract

Statistical design of experiments (DOE) was used to rapidly optimize Red-Al reduction of an imide to produce, after deprotection and salt formation, 3, 4-isopropylidenedioxypyrrolidine hydrotosylate (1), an intermediate in the synthesis of Ingliforib. A Red-Al reduction process was successfully scaled to produce multikilogram quantities of 1, thus demonstrating a safer and more economical process. Further development resulted in an optimized procedure, ...