吡嗪置于cadmium(II) Chloride-N,N,N',N'-Tetramethylethylenediamine,2,2,6,6-Tetramethylpiperidinyl-Lithium,碘体系中,用 四氢呋喃 用作溶剂,化学反应 2.0H,以63%的收率获得2-碘吡嗪 参考文献:Synthesis Of 2,5-Diiodopyrazine By Deprotonative Dimetalation Of Pyrazine 标题:Synthesis Of 2,5-Diiodopyrazine By Deprotonative Dimetalation Of Pyrazine 摘要:室温下,在四氢呋喃中使用三(2,2,6,6-四甲基哌啶)镉锂对嘧啶和吡嗪进行了区域选择性脱金属反应.随后用碘进行捕集,得到了 4-碘嘧啶和 2-碘吡嗪,产率分别为 71% 和 63%.对哒嗪进行同样的反应,可得到 3-碘和 4-碘衍生物的混合物(产率分别为 55% 和 41%).事实证明,从吡嗪中获得 2,5-二碘衍生物(在 25 毫摩尔的规模上为 40%)需要使用更大量的碱(1 等量而不是 0.33). Doi:10.1055/s-0028-1083218
专利信息
专利号:US-11512097-B2 优先权日:2019-11-25 标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use 发明人:ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO 权利人:AMGEN INC 摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-8404670-B2 优先权日:2009-02-11 标题:Histamine H3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:CN-111039910-A 优先权日:2019-12-31 标题 :A kind of method and application of photo-initiated synthesis of 3-aryl flavonoids or coumarin compounds
专利号:CN-115557905-A 优先权日:2022-08-31 标 题 :A new green method for preparing aminopyrazine and its use in the synthesis of pharmaceutical intermediates
专利号:CN-115557905-B 优先权日:2022-08-31 标 题:A new green method for preparing aminopyrazine and its application in the synthesis of pharmaceutical intermediates
专利号:US-2013150376-A1 优先权日:2010-04-09 标 题:Novel Sultam Compounds 发明人:BRODNEY MICHAEL AARON; EFREMOV IVAN VIKTOROVICH; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS 权利人:BRODNEY MICHAEL AARON; EFREMOV IVAN VIKTOROVICH; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS; PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.