欧盟法规
ECHA物质C&L通报上下游产品
2-氨基-3-溴-5-甲基吡嗪 3-Bromo-5-Methylpyrazin-2-Amine 74290-65-62-氨基-3-溴-5-甲基吡嗪置于palladium On Activated Charcoal 氢气,三乙胺体系中,用 乙酸乙酯 作为反应溶剂,化学反应 0.33H,以98%的收率获得产物2-氨基-5-甲基吡嗪
参考文献:Sato,Nobuhiro,Journal Of Heterocyclic Chemistry,1980,Vol. 17,P. 143-147
标题:Sato,Nobuhiro,Journal Of Heterocyclic Chemistry,1980,Vol. 17,P. 143-147
专利信息
专利号:US-8207337-B2
优先权日:2007-01-29
标 题:Reagent for organic synthesis reaction containing organic triol borate salt
发明人:MIYAURA NORIO; YAMAMOTO YASUNORI
权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD
摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).
专利号:US-10975101-B2
优先权日:2016-05-31
标题:Ultra-potent vinca alkaloids: added molecular complexity further disrupts the tublin dimer-dimer interface
发明人:BOGER DALE
权利人:SCRIPPS RESEARCH INST
摘要:Synthetically-derived and previously inaccessible modifications of 20′-hydroxy-vinca derivative compounds such as vinblastine, vincristine or vindesine are disclosed that are a stunning 100-fold more active than the natural product (IC 50 's 50-75 pM vs 7 nM, HCT116), and are now accessible as a result of advances in the total synthesis of the natural product. Illustrative new ultra-potent vinblastines bind tubulin with much higher affinity and likely further disrupt the tubulin head-to-tail α/β dimer-dimer interaction by virtue of the strategic placement of an added conformationally well-defined, rigid and extended C20′-urea along the adjacent protein-protein interface. Added molecular complexity was used to markedly enhance target binding and functional biological activity, and represents a general approach to improving the properties of other natural products targeting a protein-protein interaction. A pharmaceutical composition containing an ultra-potent 20′-hydroxy-vinca derivative compound and a method of treating cancerous cells with such a compound are also disclosed.
专利号:GB-596868-A
优先权日:1944-01-20
标 题 :Improvements in or relating to the synthesis of sulphonamide compounds
专利号:US-11731956-B2
优先权日:2018-10-22
标 题:Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors