CAS: 868963-98-8; 2-Amino-5-Bromopyridine-3-Sulfonyl Chloride

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CAS号1072-97-5 2-氨基-5-溴吡啶 | CAS号7790-94-5 氯磺酸 | CAS号38875-53-5 5-溴-2,3-二氨基吡啶

📜2,3-二氨基-5-溴吡啶置于盐酸,Sodium Nitrite,二氧化硫,溶剂黄146,Copper(L) Chloride体系中,用 水 作为反应溶剂,化学反应 3.25H,反应生成 2-氨基-5-溴吡啶-3-磺酰氯
参考文献:Discovery Of A Novel Series Of Potent And Orally Bioavailable Phosphoinositide 3-Kinase γ Inhibitors
标题:Discovery Of A Novel Series Of Potent And Orally Bioavailable Phosphoinositide 3-Kinase γ Inhibitors
摘要:The Phosphoinositide 3-Kinases (Pi3Ks) Have Been Linked To An Extraordinarily Diversified Group Of Cellular Functions Making These Enzymes Compelling Targets For The Treatment Of Disease. A Large Body Of Evidence Has Linked Pi3K Gamma To The Modulation Of Autoimmune And Inflammatory Processes Making It An Intriguing Target For Drug Discovery. Our High-Throughput Screening (Hts) Campaign Revealed Two Hits That Were Nominated For Further Optimization Studies. The In Vitro Activity Of The First Hts Hit,Designated As The Sulfonylpiperazine Scaffold,Was Optimized Utilizing Structure-Based Design. However,Nonoptimal Pharmacokinetic Properties Precluded This Series From Further Studies. An Overlay Of The X-Ray Structures Of The Sulfonylpiperazine Scaffold And The Second Hts Hit Within Their Complexes With Pi3K Gamma Revealed A High Degree Of Overlap. This Feature Was Utilized To Design A Series Of Hybrid Analogues Including Advanced Leads Such As 31 With Desirable Potency,Selectivity,And Oral Bioavailability.
DOI:10.1021/jm300403A