N-(4-Fluoro-2-Methylphenyl)-2-Methylpropane-2-Sulfinamide置于盐酸,碳酸氢钠体系中,用 1,4-二氧六环,水 作为反应溶剂,化学反应 0.25H,以96%的收率获得产物4-氟-2-甲基苯胺 参考文献:Efficient Indoles And Anilines Syntheses Employing Tert-Butyl Sulfinamide As Ammonia Surrogate 标题:Efficient Indoles And Anilines Syntheses Employing Tert-Butyl Sulfinamide As Ammonia Surrogate 摘要:Tert-Butyl Sulfinamide Is An Ammonia Equivalent For The Palladium-Catalyzed Amination Of Aryl Bromides And Aryl Chlorides. Using These Amine Derivatives,It Has Been Observed That Indoles And Anilines With Sensitive Functional Groups Can Be Readily Prepared. This Surrogate Has Also Been Used For The Synthesis Of Indoles From 2-Halophenols Using Palladium Catalyzed Cross Coupling Reaction As The Key Step. (C) 2011 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Tetlet.2011.08.075
专利号:US-7897762-B2 优先权日:2006-09-14 标 题:Kinase inhibitors useful for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:DECIPHERA PHARMACEUTICALS LLC 摘要:The present invention relates to novel kinase inhibitors and modulator compounds 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-5998595-A 优先权日:1996-11-05 标题:Azidohalogenobenzyl derivatives, sugar compounds and protection of hydroxy groups 发明人:KUSUMOTO SHOICHI; FUKASE KOICHI 权利人:WAKO PURE CHEM IND LTD 摘要:Azidohalogenobenzyl derivatives of the formula (I) ##STR1## wherein A is a halogen atom, B is a halogen atom or a hydrogen atom, and X is a group reactive with a hydroxy group, methods of protecting hydroxy group(s) using said derivatives, and sugar compounds wherein a hydrogen atom of at least one hydroxy group is substituted by an azidohalogenobenzyl group. According to the present invention, there are provided novel derivatives capable of introducing a group into a compound having hydroxy group(s), which group is useful as a stable hydroxy-protecting group even in solid phase synthesis for the purpose of the extension of sugar chain under continuous acidic conditions and of being removed under mild conditions; sugar compounds protected by using said derivatives; and methods of protecting hydroxy group(s) using said derivatives.
专利号:US-2005026965-A1 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of nicotinanilide-N-oxides
专利号:US-2023104311-A1 优先权日:2020-02-17 标题:Novel 6-substituted 7-deazapurines and corresponding nucleosides as medicaments 发明人:HERDEWIJN PIET; GROAZ ELISABETTA; QINGFENG LI 权利人:UNIV LEUVEN KATH 摘要:The present invention relates to the synthesis of 6-substituted 7-deazapurines and their corresponding nucleosides by coupling aryl or alkyl Grignard reagents with halogenated purine nucleosides in the presence of iron or an iron/copper mixture such as Fe(acac)3/CuI. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections.
专利号:US-2003004189-A1 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of nicotinanilide-N-oxides
专利号:US-2010063105-A1 优先权日:2000-12-29 标题 :Pharmaceutical uses and synthesis of nicotinanilide-n-oxides
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 176. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 80.