312904-12-4Relevant articles and documents
Preparation method of oseltamivir
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Paragraph 0075; 0078; 0079, (2020/08/22)
The invention discloses a preparation method of oseltamivir. The preparation method comprises the steps: taking (1S,5R,6S)-5-(pentan-3-yloxy)-7-oxabicyclo[4.1.0]hept-3-ene-3-carboxylic acid ethyl ester as a raw material; carrying out a ring-opening reaction with benzylamine, carrying out catalytic hydrogenation debenzylation protection, carrying out Boc-protected N-acylation, carrying out an O-sulfonylation reaction with substituted sulfonyl chloride or trifluoromethanesulfonic anhydride, and carrying out a substitution reaction with benzylamine; carrying out catalytic hydrogenation debenzylation protection and O-acetylation reaction again; and finally removing Boc protection under an acidic condition to prepare oseltamivir. The preparation process is simple, low in cost and suitable for process amplification preparation to meet industrial production of oseltamivir raw drugs.
Process for the preparation of 4,5-diamino shikimic acid derivatives
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Page/Page column 6, (2008/06/13)
The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula and pharmaceutically acceptable addition salts thereof wherein R1, R1′ are independent of each other H or alkyl, R2 is an alkyl and R3, R4 are independent of each other H or an alkanoyl, with the proviso that not both R3 and R4 are H. 4,5-diamino shikimic acid derivatives of formula I, especially the (3R,4R,5S)-5-amino-4-acetylamino-3-(1-ethyl-propoxy)-cyclohex-1-ene-carboxylic acid ethyl ester and its pharmaceutically acceptable additional salts are potent inhibitors of viral neuraminidase.
Process for preparing 1,2-diamino compounds
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, (2008/06/13)
The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.