Invention Grant
- Patent Title: Regioselective acylation of rapamycin at the C-42 position
- Patent Title (中): 雷帕霉素在C-42位置的区域选择性酰化
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Application No.: US14005678Application Date: 2012-03-30
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Publication No.: US09051336B2Publication Date: 2015-06-09
- Inventor: Wolfgang Felzmann , Niklas Schone
- Applicant: Wolfgang Felzmann , Niklas Schone
- Applicant Address: CH Basel
- Assignee: SANDOZ
- Current Assignee: SANDOZ
- Current Assignee Address: CH Basel
- Agency: Manelli Selter PLLC
- Agent Jeffrey S. Melcher
- Priority: EP11160858 20110401
- International Application: PCT/EP2012/055757 WO 20120330
- International Announcement: WO2012/131019 WO 20121004
- Main IPC: C07D498/18
- IPC: C07D498/18 ; C07D498/14
Abstract:
The invention refers to the selective acylation of Rapamycin at the 42-position (I) with an acylating agent of the formula (II) wherein R4 and R5 are the same or different, individually the rest of an acetal, especially tetrahydropyran, or of a carbonate or the rest of a silyl ether or taken together are the rest of a boronate, an acetal or ketal.
Public/Granted literature
- US20140081016A1 REGIOSELECTIVE ACYLATION OF RAPAMYCIN AT THE C-42 POSITION Public/Granted day:2014-03-20
Information query
