Process for preparing pergolide

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United States of America Patent

PATENT NO 6388079
SERIAL NO

09651381

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Abstract

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This invention relates to a process for preparing pergolide, which comprises the steps of reacting 9,10-dihydrolysergol with an acid anhydride at an elevated temperature in the presence of a catalyst to form a triacylated product intermediate; reducing the triacylated product intermediate with a reducing agent in a solvent to form a primary amino alcohol intermediate; and reacting the amino alcohol intermediate with dimethyl disulfide and trialkyl phosphine, aryl phosphine or the polymeric derivatives of phosphine analogs thereof in a polar solvent to obtain pergolide; or the steps of reacting 9,10-dihydrolysergol with dimethyl disulfide and trialkyl phosphine, aryl phosphine or the polymeric derivatives of phosphine analogs thereof in a polar solvent to form a methylsulfide intermediate; reacting the methylsulfide intermediate with an acid anhydride at an elevated temperature in the presence of a catalyst to form a diacylated amide intermediate; and reducing the diacylated amide intermediate with a reducing agent in a solvent to obtain pergolide.

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Patent Owner(s)

Patent OwnerAddress
SCINOPHARM SINGAPORE PTE LTD168 ROBINSON ROAD #25-01 CAPITAL TOWER SINGAPORE

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Wu, Edwin S C Tainan, TW 10 31
Wu, Mark Taipei Hsien, TW 18 284

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