发明名称 PREPARATION OF NEURAMINIDASE INHIBITOR
摘要 PROBLEM TO BE SOLVED: To obtain a specific diamino compound useful as a viral or bacterial neuraminidase inhibitor without using an azide reagent and azide intermediate through various reactions such as reaction between a specific epoxide and specific amine. SOLUTION: This compound of formula V is obtained by such processes that a compound of formula I (R1, R1', R2, and R2' are each H, an alkyl or the like, but only one of them is H) is reacted with a compound of the formula R5NHR6 (R5 and R6 are each H or an amino substituent, but both of them is not H at the same time) to form a compound of formula II, which is converted to a compound of formula III, which is converted to a compound of formula IV; the free-amino functional group at position 1 of the compound of formula IV is acylated to form the corresponding acylated 1,2-diamino compound and then the amino group at position 2 of the above diamino compound is freed; if necessary, the compound of formula V (R3 and R4 are each H or an amino substituent but both of them are not H at the same time) thus obtained is further converted to the corresponding pharmaceutically acceptable addition salt.
申请公布号 JP2001031631(A) 申请公布日期 2001.02.06
申请号 JP20000171482 申请日期 2000.06.08
申请人 F HOFFMANN LA ROCHE AG 发明人 KARPF MARTIN;TRUSSARDI RENE
分类号 B01J31/12;C07B61/00;C07C209/14;C07C209/16;C07C209/52;C07C211/25;C07C211/36;C07C211/40;C07C213/04;C07C213/08;C07C215/20;C07C217/52;C07C231/12;C07C233/03;C07C233/41;C07C233/52;C07C309/66;C07C317/48;C07C317/50;(IPC1-7):C07C209/16 主分类号 B01J31/12
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