Invention Grant
US08686141B2 Process for preparing N-substituted hydroxypyrimidinone carboxamides
有权
制备N-取代羟基嘧啶酮甲酰胺的方法
- Patent Title: Process for preparing N-substituted hydroxypyrimidinone carboxamides
- Patent Title (中): 制备N-取代羟基嘧啶酮甲酰胺的方法
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Application No.: US12811254Application Date: 2008-12-22
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Publication No.: US08686141B2Publication Date: 2014-04-01
- Inventor: Guy R. Humphrey , Ross A. Miller , Peter E. Maligres , Steven Weissman
- Applicant: Guy R. Humphrey , Ross A. Miller , Peter E. Maligres , Steven Weissman
- Applicant Address: US NJ Rahway
- Assignee: Merck Sharp & Dohme Corp.
- Current Assignee: Merck Sharp & Dohme Corp.
- Current Assignee Address: US NJ Rahway
- Agent Jeffrey P. Bergman; Sheldon O. Heber
- International Application: PCT/US2008/087929 WO 20081222
- International Announcement: WO2009/088729 WO 20090716
- Main IPC: C07D239/52
- IPC: C07D239/52 ; C07D413/12

Abstract:
Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.
Public/Granted literature
- US20100280244A1 PROCESS FOR PREPARING N-SUBSTITUTED HYDROXYPYRIMIDINONE CARBOXAMIDES Public/Granted day:2010-11-04
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