📜5-溴-1-甲基吲哚置于正丁基锂,硼酸三丁酯体系中,用 四氢呋喃 用作溶剂,化学反应 0.75H,以33.33%的收率获得1-甲基吲哚-5-硼酸 参考文献: Spiro-Substituted Oxindole Derivatives Having Ampk Activity[fr] Dérivés D'Oxindole Spiro-Substitués Ayant Une Activité Sur Ampk 标题: Spiro-Substituted Oxindole Derivatives Having Ampk Activity[fr] Dérivés D'Oxindole Spiro-Substitués Ayant Une Activité Sur Ampk 摘要:本发明涉及具有有价值的药理特性的式(I)化合物,特别是ampk激活剂,因此在治疗某些可以通过激活该受体预防或治疗的疾病方面具有用处.这些化合物适用于治疗和预防可以受该受体影响的疾病,如代谢性疾病,特别是2型糖尿病.
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-2009137557-A1 优先权日:2005-11-22 标题 :Calcilytic Compounds 发明人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 权利人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
专利号:US-2016229847-A1 优先权日:2013-10-04 标 题:Novel bicyclic pyridinones as gamma-secretase modulators 发明人:PETTERSSON MARTIN YOUNGJIN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; JOHNSON DOUGLAS SCOTT; KAUFFMAN GREGORY WAYNE; O'DONNELL CHRISTOPHER WILLIAM; PATEL NANDINI CHATURBHAI; STEPAN ANTONIA FRIEDERIKE; STIFF CORY MICHAEL; SUBRAMANYAM CHAKRAPANI; TRAN TUAN PHONG; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula II as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
参考标题:Synthesis Of New Heteroaryl Substituted Morpholine Tagged Triazines And Evaluation Of Their Cytotoxic Activity 作者:Sivaprasad Kasturi,Sujatha Surarapu,Srinivas Uppalanchi,Hasitha Shilpa Anantaraju,Shubham Dwivedi,Perumal Yogeeswari,Krishna S. Ethiraj,Jaya Shree Anireddy |发布日期:2018.1.30 摘要:Background: In The Present Study, New Triazine Derivatives 3, 4, 5, 6, 8 And 10 Were Synthesized Starting From Readily Available Cyanuric Chloride 1 Via Nucleophilic Displacement With Morpholine Followed By Suzuki Or Stille Coupling Reactions And Then The Thermal Displacement Of Chlorine Atom With Diverse Substituted Amines. Methods: All Synthesized Compounds Were Screened For Their Cytotoxic Activity
合成参考文献
摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2018) 3, 168. 摘要:Croft, R. A.; Bull, J. A., Science of Synthesis Knowledge Updates, (2018) 4, 419. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 68. 摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 239. 摘要:Xiao, X., Science of Synthesis: Knowledge Updates, (2023) 2, 199.