Synthesis of Rofecoxib, (MK 0966, Vioxx 4-(4'-Methylsulfonylphenyl)-3-Phenyl-2(5H)-Furanone), a Selective and Orally Active Inhibitor of Cyclooxygenase-2

Michel Therien; Jacques Yves Gautheir; Yves Leblanc

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Synthesis of Rofecoxib, (MK 0966, Vioxx 4-(4'-Methylsulfonylphenyl)-3-Phenyl-2(5H)-Furanone), a Selective and Orally Active Inhibitor of Cyclooxygenase-2

机译：罗非考昔（MK 0966，Vioxx 4-（4'-甲基磺酰基苯基）-3-苯基-2（5H）-呋喃酮）的合成，环氧化酶2的选择性和口服活性抑制剂

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摘要

The synthesis of Vioxx (Rofecoxib, MK 966, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone), a newly FDA approved inhibitor of cyclooxygenase-2, is described.

机译：描述了新获FDA批准的环氧合酶2抑制剂Vioxx（Rofecoxib，MK 966，4-（4'-甲基磺酰基苯基）-3-苯基-2（5H）-呋喃酮）的合成。

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《Synthesis: International Journal of Methods in Synthetic Organic Chemistry》 |2001年第12期|共2页
作者
Michel Therien; Jacques Yves Gautheir; Yves Leblanc;
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正文语种 eng
中图分类有机化学;
关键词
lactones; sulfones; anti-inflammatory drugs;

机译：内酯;砜;抗炎药;

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1. Synthesis of Rofecoxib, (MK 0966, Vioxx 4-(4'-Methylsulfonylphenyl)-3-Phenyl-2(5H)-Furanone), a Selective and Orally Active Inhibitor of Cyclooxygenase-2 [J] . Michel Therien, Jacques Yves Gautheir, Yves Leblanc Synthesis: International Journal of Methods in Synthetic Organic Chemistry . 2001,第12期

机译：罗非考昔（MK 0966，Vioxx 4-（4'-甲基磺酰基苯基）-3-苯基-2（5H）-呋喃酮）的合成，环氧化酶2的选择性和口服活性抑制剂
2. The discovery of rofecoxib, (MK 966, Vioxx, 4-(4'-methylsulfonylphenyl)-3-phenyl-2(5H)-furanone), an orally active cyclooxygenase-2-inhibitor. [J] . Prasit P, Wang Z, Brideau C, Bioorganic and Medicinal Chemistry Letters . 1999,第13期

机译：口服活性环加氧酶-2-抑制剂罗非昔布（MK 966，Vioxx，4-（4'-甲基磺酰基苯基）-3-苯基-2（5H）-呋喃酮）的发现。
3. Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx). [J] . Nicoll-Griffith DA, Yergey JA, Trimble LA, Bioorganic and Medicinal Chemistry Letters . 2000,第23期

机译：衍生自环加氧酶2抑制剂rofecoxib（MK-0966，Vioxx）的代谢物的合成，表征和活性。
4. The Cyclooxygenase-2 Selective Inhibitor Celecoxib Suppresses Proliferation and Invasiveness in the Human Oral Squamous Carcinoma [C] . YOUNG EUN KWAK, NAM KYEOUNG JEON, JIN KIM, Meeting on Cell Signaling World: Signal Transduction Pathways as Therapeutic Targets . 2007

机译：环氧合酶2选择性抑制剂塞来昔布抑制人口腔鳞状细胞癌的增殖和侵袭。
5. Part One. Synthesis of optically active tryptophan derivatives with potential activity as indoleamine 2,3-dioxygenase inhibitors: An approach via asymmetric catalytic hydrogenation. Part Two. Design, synthesis and pharmacology of selective ligands for alpha1-containing GABA(A)/benzodiazepine receptor subtypes: SAR studies of beta-carbolines at positions -3 and -6 and their corresponding bivalent ligands. Part Three. First enantiospecific total synthesis of the important biogenetic intermediates, (+)-polyneuridine and (+)-polyneuridine aldehyde, as well as 16-epi-vellosimine and macusine A. [D] . Yin, Wenyuan. 2007

机译：第一部分。具有吲哚胺2,3-二加氧酶抑制剂潜在活性的旋光色氨酸衍生物的合成：一种通过不对称催化氢化的方法。第二部分。含α1的GABA（A）/苯并二氮杂receptor受体亚型的选择性配体的设计，合成和药理作用：位于-3和-6位的β-咔啉及其相应的二价配体的SAR研究。第三部分。重要生物遗传中间体，（+）-聚神经氨酸和（+）-聚神经氨酸醛，以及16-表-维西辛和Macusine A的首次对映体全合成。
6. Effects of rofecoxib a selective cyclooxygenase-2 inhibitor on endothelial dysfunction lipid peroxidation and hepatocyte morphology in rats with sepsis-induced liver damage [O] . Eray Kara, Ahmet Var, Seda Vatansever, 2004

机译：选择性环氧合酶2抑制剂罗非考昔对败血症诱发的肝损伤大鼠内皮功能脂质过氧化和肝细胞形态的影响
7. Novel Potent Orally Active Selective VEGFR-2 Tyrosine Kinase Inhibitors: Synthesis, Structure-Activity Relationships, and Antitumor Activities of N-Phenyl-N-{4-(4-quinolyloxy)phenyl}ureas [O] . -1

机译：新型有效口服活性选择性选择性VEGFR-2酪氨酸激酶抑制剂：N-苯基-N- {4-（4-喹啉氧基）苯基}脲的合成，结构活性关系和抗肿瘤活性

Synthesis of Rofecoxib, (MK 0966, Vioxx 4-(4'-Methylsulfonylphenyl)-3-Phenyl-2(5H)-Furanone), a Selective and Orally Active Inhibitor of Cyclooxygenase-2

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