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Title:
3-オキシイミノステロイドの調製方法
Document Type and Number:
Japanese Patent JP2007508380
Kind Code:
A
Abstract:
The present invention provides a method of preparing norelgestromin or norgestimate by reacting the corresponding 3-oxosteroid precursor with hydroxylamine HCl and a base to obtain a reaction mixture forming norelgestromin or norgestimate; monitoring the anti/syn ratio of the norelgestromin or norgestimate produced in the reaction mixture; adding a base to the reaction mixture to neutralize acidity in the reaction mixture when a desired anti/syn ratio is detected; and isolating the norelgestromin or norgestimate. The present invention also provides a process allowing a control of the formation of the anti isomer and syn isomer of norelgestromin or norgestimate by reacting the corresponding 3-oxosteroid precursor with hydroxylamine HCl and a base to obtain a reaction mixture forming norelgestromin or norgestimate; regulating the acidity of the reaction mixture to adjust the anti/syn ratio of the norelgestromin or norgestimate produced in the reaction mixture; adding a base to the reaction mixture to neutralize acidity in the reaction mixture when a desired anti/syn ratio is detected; and isolating the norelgestromin or norgestimate.

Inventors:
Villa, Marco
Fretta, Roberta
Nikola, Diurgerov
Application Number:
JP2006535474A
Publication Date:
April 05, 2007
Filing Date:
August 12, 2005
Export Citation:
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Assignee:
Sicole Incorporated
International Classes:
C07J7/00
Domestic Patent References:
JPS624400B21987-01-30
Foreign References:
WO2005000867A12005-01-06
GB1123104B
Attorney, Agent or Firm:
Atsushi Aoki
Takashi Ishida
Fukumoto product
Tetsuji Koga
Kazuhiro Nakamura