Chemical development of MDL 103371: an N-Methyl-D-aspartate-type glycine receptor antagonist for the treatment of stroke

…, RA Schnettler, CR Nevill, FJ Weiberth…

Index: Watson, Timothy J.N.; Horgan, Stephen W.; Shah, Ramnik S.; Farr, Robert A.; Schnettler, Richard A.; Nevill Jr., C. Richard; Weiberth, Franz J.; Huber, Edward W.; Baron, Bruce M.; Webster, Mark E.; Mishra, Rajesh K.; Harrison, Boyd L.; Nyce, Phillip L.; Rand, Cynthia L.; Goralski, Christian T. Organic Process Research and Development, 2000 , vol. 4, # 6 p. 477 - 487

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Citation Number: 27

Abstract

MDL 103371 is a N-methyl-d-aspartate (NMDA)-type glycine receptor antagonist for the potential treatment of stroke. Evaluation of five different synthetic routes, which included Stille, Suzuki, enol ether, Knoevenagel, and the Mukaiyama coupling reactions, revealed the Knoevenagel approach superior for preparing large quantities of drug substance for evaluation. The overall process utilized some classical chemistry. Fischer indole ...