2-<(tert-Butoxycarbonyl)amino>-5-hydroxy-L-valeric acid | 83345-45-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-<(tert-Butoxycarbonyl)amino>-5-hydroxy-L-valeric acid
• 英文别名: Boc-L-pentahomoserine；2-[(tert-Butoxycarbonyl)amino]-5-hydroxy-L-valeric acid；(S)-2-((tert-Butoxycarbonyl)amino)-5-hydroxypentanoic acid；(2S)-5-hydroxy-2-[(2-methylpropan-2-yl)oxycarbonylamino]pentanoic acid
• CAS: 83345-45-3
• 化学式: C₁₀H₁₉NO₅
• 分子量: 233.265
• InChiKey: XKNSMPKNTBHIIH-ZETCQYMHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  16
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  95.9
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-<(tert-Butoxycarbonyl)amino>-5-hydroxy-L-valeric acid 在 甲酸 作用下， 反应 4.0h， 生成 2-氨基-5-羟基-戊酸
  参考文献：
  名称：

  Micropeptins from the Freshwater Cyanobacterium Microcystis aeruginosa (NIES-100)

  摘要：

  Micropeptins C (1), D (2), E (3), and F (4) have been isolated from the freshwater cyanobacterium Microcystis aeruginosa (NIES-100). The structures were elucidated by analyses of MS, NMR spectra, and chemical degradation. Micropeptins C, D, E, and F inhibited chymotrypsin with IC50's of 1.1, 1.2, 1.0, and 1.5 mu g/mL, respectively.

  DOI：

  10.1021/np800631t
• 作为产物：
  描述：

  Boc-L-谷氨酰胺 在 氨 、 sodium 作用下， 生成 2-<(tert-Butoxycarbonyl)amino>-5-hydroxy-L-valeric acid
  参考文献：
  名称：

  Sodium-liquid ammonia reduction of carboxamides to alcohols

  摘要：

  DOI：

  10.1021/jo00159a030

文献信息

• [EN] MYELOPEROXIDASE IMAGING AGENTS<br/>[FR] AGENTS D'IMAGERIE DE MYÉLOPEROXYDASE
  申请人：MASSACHUSETTS GEN HOSPITAL

  公开号：WO2018094005A1

  公开（公告）日：2018-05-24

  Provided herein are compounds useful as imaging agents. Exemplary compounds provided herein are useful as myeloperoxidase imaging agents using positron emission tomography or fluorescence imaging techniques. Methods for preparing the compounds provided herein and diagnostic methods using radiolabeled and unlabeled compounds are also provided.

  本文提供了作为成像剂有用的化合物。本文提供的示例化合物可用作髓过氧化物酶成像剂，使用正电子发射断层扫描或荧光成像技术。还提供了制备本文提供的化合物的方法以及使用放射标记和未标记化合物的诊断方法。
• 一种由戊高丝氨酸合成天然产物(±)- Pestaloxazine A的方法
  申请人：扬州蓝色生物医药科技有限公司

  公开号：CN107459526B

  公开（公告）日：2019-09-27

  本发明涉及一种由戊高丝氨酸合成天然产物(±)‑pestaloxazine A的方法，其包括由被保护的戊高丝氨酸出发经缩合、氧化、环合等系列反应得到对称双噁嗪烷螺二酮哌嗪化合物A后与侧链化合物B发生缩合反应制备天然产物(±)‑pestaloxazine A的步骤：
• Omega aminoalkylamides of R-2 aryl propionic acids as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells
  申请人：Allegretti Marcello

  公开号：US20050080067A1

  公开（公告）日：2005-04-14

  (R)-2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of the chemotaxis of neutrophils and monocytes induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, rheumatoid arthritis and in the prevention and the treatment of injury caused by ischemia and reperfusion.

  本文描述了化合物公式(I)的(R)-2-Arylpropionamide化合物，以及它们的制备过程和制药制剂。发明的2-Arylpropionamides可用于预防和治疗由于炎症部位的多形核白细胞（白细胞PMN）和单核细胞的加重招募而导致的组织损伤。特别地，本发明涉及公式(I)的2-aryl丙酸的ω-氨基烷基酰胺的R对映体，用于抑制由补体的C5a分数和其他趋化蛋白引起的中性粒细胞和单核细胞趋化，并且这些趋化蛋白的生物活性与7-TD受体的激活有关。公式(I)的选定化合物是同时抑制C5a诱导的中性粒细胞和单核细胞趋化以及IL-8诱导的PMN白细胞趋化的双重抑制剂。本发明的化合物用于治疗牛皮癣、溃疡性结肠炎、肾小球肾炎、急性呼吸功能不全、特发性纤维化、类风湿性关节炎以及预防和治疗缺血再灌注引起的损伤。
• Dipeptide nitriles
  申请人：——

  公开号：US20040029814A1

  公开（公告）日：2004-02-12

  N-terminal substituted dipeptide nitrites as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitrites are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof 1 wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R 2 , R 3 , R 4 , R 5 , X 1 , Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.

  N-末端取代二肽硝酸盐可作为半胱氨酸蛋白酶的抑制剂，例如半胱氨酸蛋白酶B、K、L和S，并可用于治疗半胱氨酸蛋白酶依赖性疾病和病况，包括炎症、类风湿性关节炎、骨关节炎、骨质疏松症、肿瘤（尤其是肿瘤侵袭和转移）、冠心病、动脉粥样硬化（包括动脉粥样硬化斑块破裂和不稳定）。特定的二肽硝酸盐是化合物I的化合物，或其生理可接受和可分解的酯或盐。其中：符号如定义。特别是通过适当选择R、R2、R3、R4、R5、X1、Y和L的基团，可以改变化合物作为各种半胱氨酸蛋白酶类型的抑制剂的相对选择性，例如半胱氨酸蛋白酶B、K、L和S，以获得选择性抑制特定半胱氨酸蛋白酶类型或半胱氨酸蛋白酶类型组合的抑制剂。
• Antibacterial amide macrocycles VI
  申请人：Endermann Rainer

  公开号：US20080300231A1

  公开（公告）日：2008-12-04

  The invention relates to antibacterial amide macrocycles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular of bacterial infections.

  本发明涉及抗菌酰胺大环化合物及其制备方法，以及它们用于治疗和/或预防疾病的用途，以及它们用于制备治疗和/或预防疾病的药物，特别是细菌感染的药物。