CAS: 916791-10-1; [1-(4-Chloropyrimidin-2-yl)Piperidin-3-Yl]Methanol

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3-(hydroxymethy)piperidine 2,6-Dichloropyrimidine

📜3-哌啶甲醇,2,4-二氯嘧啶置于三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 2.0H,反应生成 1-(4-氯-2-嘧啶基)-3-哌啶甲醇,[1-(2-Chloropyrimidin-4-yl)Piperidin-3-Yl]Methanol
参考文献:Discovery Of The Macrocycle (9E)-15-(2-(Pyrrolidin-1-yl)Ethoxy)-7,12,25-Trioxa-19,21,24-Triaza-Tetracyclo[18.3.1.1(2,5).1(14,18)]Hexacosa-1(24),2,4,9,14(26),15,17,20,22-Nonaene (Sb1578),A Potent Inhibitor Of Janus Kinase 2/fms-Liketyrosine Kinase-3 (Jak2/flt3) For The Treatment Of Rheumatoid Arthritis
标题:Discovery Of The Macrocycle (9E)-15-(2-(Pyrrolidin-1-yl)Ethoxy)-7,12,25-Trioxa-19,21,24-Triaza-Tetracyclo[18.3.1.1(2,5).1(14,18)]Hexacosa-1(24),2,4,9,14(26),15,17,20,22-Nonaene (Sb1578),A Potent Inhibitor Of Janus Kinase 2/fms-Liketyrosine Kinase-3 (Jak2/flt3) For The Treatment Of Rheumatoid Arthritis
摘要:Herein,We Describe The Synthesis And Sar Of A Series Of Small Molecule Macrocycles That Selectively Inhibit Jak2 Kinase Within The Jak Family And Flt3 Kinase. Following A Multiparameter Optimization Of A Key Aryl Ring Of The Previously Described Sb1518 (Pacritinib),The Highly Soluble 141 Was Selected As The Optimal Compound. Oral Efficacy In The Murine Collagen-Induced Arthritis (Cia) Model For Rheumatoid Arthritis (Ra) Supported 141 As A Potential Treatment For Autoimmune Diseases And Inflammatory Disorders Such As Psoriasis And Ra. Compound 141 (Sb1578) Was Progressed Into Development And Is Currently Undergoing Phase 1 Clinical Trials In Healthy Volunteers.
DOI:10.1021/jm201454N