| 1315306-49-0

• 分子结构分类: 有机化合物 - 有机杂环化合物
• CAS: 1315306-49-0
• 化学式: C₂₃H₂₄NO₅PS
• 分子量: 457.487
• InChiKey: ZDHSHVQBBBYVMR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  None
• 重原子数：
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• 可旋转键数：
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• 环数：
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• sp3杂化的碳原子比例：
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• 拓扑面积：
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• 氢给体数：
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• 氢受体数：
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文献信息

• Synthesis and Evaluation of Bombesin Analogues Conjugated to Two Different Triazolyl-Derived Chelators for 99mTc Labeling
  作者：Luc Brans、Elisa García-Garayoa、Christian Schweinsberg、Veronique Maes、Harriet Struthers、Roger Schibli、Dirk Tourwé

  DOI：10.1002/cmdc.201000191

  日期：——

  fairly lipophilic, radiolabeled peptide can be enhanced by glycation, which is easily carried out by CuI‐catalyzed cycloaddition. Herein, we further elaborate this “click approach” in the synthesis of a new series of triazole‐based chelating systems as alternatives to the (NαHis)Ac chelator for labeling with the 99mTc(CO)3 core. The bombesin analogues, containing these new chelating systems, were evaluated

  胃泌素释放肽受体（GRPR）的过表达在多种人类癌症中提供了诊断和治疗的手段。先前我们报道了代谢稳定（ Ñ α氨酸）的Ac-βAla-βAla-[查13，NLE 14 ] BBS（7-14）类似物与用于GRPR高亲和性。我们还表明，这种相当亲脂性的，放射性标记的肽的生物分布模式可以通过糖化作用增强，这可以通过Cu I催化的环加成反应轻松实现。在此，我们进一步阐述在一系列新的合成这个“点击的方法”三唑系螯合剂系统以替代所述（ Ñ α His）的AC螯合剂用于与标记99米TC（CO）3芯。铃蟾肽类似物，含有这些新螯合剂系统，分别相对于它们的合成和体外和体内性质评价，并进行了比较用它们的（ Ñ α His）的AC对应。螯合剂对生物分布特性的影响小于糖基化，这明显改善了肿瘤与背景的比率。
• Novel aminophosphonothiophene derivatives from β-keto-δ-carbethoxyphosphonates and phosphineoxides
  作者：Emna Chebil、Moufida Chamakhi、Soufiane Touil

  DOI：10.1080/17415993.2011.570763

  日期：2011.6.1

  The reaction of -keto--carbethoxyphosphonates and phosphineoxides with active methylene nitriles leads to the corresponding phosphonoalkylidenes. Treatment of these compounds with sulfur, under the classical Gewald reaction conditions, gives a ca. 1:1 mixture of novel aminophosphonothiophene derivatives 3 and 3'. In order to improve the regioselectivity of the reaction, novel conditions have been developed for the Gewald condensation, in which we used an inorganic base NaH in THF as the solvent. These conditions afforded exclusively the 3-regioisomer in good yield. [image omitted].