CAS: 2172870-89-0; Paltusotine

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    📜3-溴-2-氟苯腈 在 盐酸,4-二甲氨基吡啶,四(三苯基膦)钯,Potassium Hydrogen Difluoride,1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,二氯双[二叔丁基-(4-二甲基氨基苯基)膦]钯(II),Potassium Acetate,碳酸氢钠,Potassium Carbonate体系中,用 2-甲基四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷,水,二甲基亚砜,异丙醇作为反应溶剂,反应 89.5H,获得 Paltusotine
    参考文献:Process Of Making Somatostatin Modulators
    标题:Process Of Making Somatostatin Modulators
    摘要:本文描述了一些肽类抑制素调节剂化合物,制备这类化合物的方法,包含这类化合物的药物组合物和药物,以及利用这类化合物治疗需要调节肽类抑制素活性的疾病,症状或疾病的方法.

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    主要参考文献


    1: Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z. Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine. Nat Commun. 2023 Feb 21;14(1):962. doi: 10.1038/s41467-023-36673-z.
    2: Zhao J, Wang S, Markison S, Kim SH, Han S, Chen M, Kusnetzow AK, Rico- Bautista E, Johns M, Luo R, Struthers RS, Madan A, Zhu Y, Betz SF. Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist. ACS Med Chem Lett. 2022 Dec 10;14(1):66-74. doi: 10.1021/acsmedchemlett.2c00431.
    3: McLaren DS, Murray RD. Paltusotine, a novel oral somatostatin receptor ligand in the management of acromegaly. J Clin Endocrinol Metab. 2022 Dec

    合成参考文献


    参考文献:10.1016/j.beem.2024.101906
    摘要:Wildemberg LE, Fialho C, Gadelha MR. Treatment of acromegaly with the nonpeptide, highly selective somatostatin receptor type 2 agonist paltusotine. Best Practice & Research Clinical Endocrinology & Metabolism. 2024 Jul;38(4):101906. doi: 10.1016/j.beem.2024.101906.
    参考文献:10.1080/14737175.2024.2417419
    摘要:Lauricella E, Vilisova S, Chaoul N, Giglio A, D’Angelo G, Porta C, Cives M. The current status of somatostatin analogs in the treatment of neuroendocrine tumors and future perspectives. Expert Review of Neurotherapeutics. 2024 Oct 16;25(2):245–58. doi: 10.1080/14737175.2024.2417419.
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