发明授权
- 专利标题: Process for the preparation of macrocyclic metalloprotease inhibitors
- 专利标题(中): 制备大环金属蛋白酶抑制剂的方法
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申请号: US09329674申请日: 1999-06-10
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公开(公告)号: US06307044B1公开(公告)日: 2001-10-23
- 发明人: Roberta L. Dorow , Silvio Campagna , Pasquale N. Confalone , Fuqiang Jin , Zhe Wang
- 申请人: Roberta L. Dorow , Silvio Campagna , Pasquale N. Confalone , Fuqiang Jin , Zhe Wang
- 主分类号: C07D27302
- IPC分类号: C07D27302
摘要:
The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.
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