罗非昔布及其衍生物合成研究进展

doi:10.6023/cjoc201212050

摘要/Abstract

罗非昔布是一种新型非甾体抗炎药, 是环氧化酶抑制剂的代表性药物, 服用罗非昔布会增加患心脏病或中风的危险. 虽然罗非昔布曾由于心血管安全风险而撤市, 但其优异的镇痛抗炎活性仍然具有很大的研究价值和广阔的应用前景, 因此以罗非昔布为先导寻找具有更高药理活性或更低毒副作用的罗非昔布衍生物一度成为研究热点. 综述了罗非昔布及其衍生物的研究进展, 包括罗非昔布合成工艺的研究, 罗非昔布衍生物的合成.

关键词: 罗非昔布, 衍生物, 合成, 研究进展

Rofecoxib is a novel non-steroidal anti-inflammatory drug, which is the representative of cyclooxygenase inhibitor. Taking rofecoxib would increase the risk of heart attack or stroke risk. Although rofecoxib withdrawal from the market due to cardiovascular risk, but its excellent analgesic and anti-inflammatory activity still has great research value and broad application prospect. Therefore, rofecoxib as a lead compound, has become a focus of research, from which researchers try to find good activity and little side effects rofecoxib derivatives. The research progress of rofecoxib and its derivatives is reviewed, including synthesis of rofecoxib and its derivatives.

Key words: rofecoxib, derivative, synthesis, research progress

引用此文

刘改枝, 韩德恩, 王鹏, 刘宏民. 罗非昔布及其衍生物合成研究进展[J]. 有机化学, 2013, 33(08): 1674-1685.

Liu Gaizhi, Han Deen, Wang Peng, Liu Hongmin. Synthesis Research Progress of Rofecoxib and Its Derivatives[J]. Chin. J. Org. Chem., 2013, 33(08): 1674-1685.

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