Development of a Scalable Process for CI-1020, A Novel Endothelin Antagonist1
…, GJ Dozeman, EA Lenoir, DT Belmont…
Index: Ellis, James E.; Davis, Edward M.; Dozeman, Gary J.; Lenoir, Edward A.; Belmont, Daniel T.; Brower, Phillip L. Organic Process Research and Development, 2001 , vol. 5, # 3 p. 226 - 233
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Citation Number: 7
Abstract
The process development of a route for preparing CI-1020 on pilot-plant scale is described in 55% overall yield. Hydrocyanation conditions are described which use acetone cyanohydrin catalyzed by tetramethylammonium hydroxide and which provide the desired ketonitrile intermediate (4) in 85% yield with excellent quality. The penultimate intermediate (7), a hydroxybutenolide, is prepared in a two-step process using an aldol condensation ...
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