发明授权
- 专利标题: Process for the preparation of chemical compounds
- 专利标题(中): 化合物的制备方法
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申请号: US10258679申请日: 2002-10-25
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公开(公告)号: US06756498B2公开(公告)日: 2004-06-29
- 发明人: Russ N. Fitzgerald , David Kendall Jung , John F Eaddy
- 申请人: Russ N. Fitzgerald , David Kendall Jung , John F Eaddy
- 主分类号: C07D47104
- IPC分类号: C07D47104
摘要:
The invention provides a process for preparing a compound of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulfonyl, C1-6alkoxy substituted by one or more fluorine atoms, halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is H or phenyl substituted by SO2C1-6alkyl or SO2NH2; R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups R6, or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring R6 is halogen, C1-6alkyl, C1-6alkoxy or C1-6alkoxy substituted by one or more fluorine atoms; which comprises rearrangement of an azirine of formula (II) wherein R0 to R3 are as defined for formula (I), or a protected derivative thereof, in the presence of a catalyst and a solvent.
公开/授权文献
- US20030212275A1 PROCESS FOR THE PREPARATION OF CHEMICAL COMPOUNDS 公开/授权日:2003-11-13
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