Invention Grant
- Patent Title: Alternative synthesis of renin inhibitors and intermediates thereof
- Patent Title (中): 肾素抑制剂及其中间体的替代合成
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Application No.: US13022243Application Date: 2011-02-07
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Publication No.: US08143416B2Publication Date: 2012-03-27
- Inventor: Gottfried Sedelmeier , Stuart John Mickel , Heinrich Rueeger
- Applicant: Gottfried Sedelmeier , Stuart John Mickel , Heinrich Rueeger
- Applicant Address: CH Basel
- Assignee: Novartis AG
- Current Assignee: Novartis AG
- Current Assignee Address: CH Basel
- Agency: Dilworth & Barrese, LLP
- Agent Ann R. Pokalsky, Esq.
- Priority: GB0419361.1 20040831
- Main IPC: C07D263/52
- IPC: C07D263/52

Abstract:
The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.
Public/Granted literature
- US20110137044A1 ALTERNATIVE SYNTHESIS OF RENIN INHIBITORS AND INTERMEDIATES THEREOF Public/Granted day:2011-06-09
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