cyclohexylmethyl 4-nitrophenyl carbonate | 176787-43-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: cyclohexylmethyl 4-nitrophenyl carbonate
• 英文别名: carbonic acid cyclohexylmethyl ester 4-nitro-phenyl ester；cyclohexylmethyl (4-nitrophenyl) carbonate
• CAS: 176787-43-2
• 化学式: C₁₄H₁₇NO₅
• 分子量: 279.293
• InChiKey: MHOQVCQZAVYWDZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  81.4
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2,3,4,6-四苄基-D-吡喃葡萄糖 、 cyclohexylmethyl 4-nitrophenyl carbonate 在 sodium hydride 作用下， 以 四氢呋喃 为溶剂， 以97%的产率得到cyclohexylmethyl [(3R,4S,5R,6R)-3,4,5-tris(phenylmethoxy)-6-(phenylmethoxymethyl)oxan-2-yl] carbonate
  参考文献：
  名称：

  通过混合碳酸盐的新型分子内脱羧糖基化

  摘要：

  已经开发出两步糖基化方法，其涉及（1）通过使用碳酸盐作为连接物来连接两个糖，（2）借助于路易斯酸去除二氧化碳以形成糖苷键。该糖基化过程基于相反的连接方式，其中糖基受体被激活以连接糖。

  DOI：

  10.1016/0040-4039(96)00272-9
• 作为产物：
  描述：

  对硝基苯基氯甲酸酯 、 苯甲醇 在 三乙胺 作用下， 生成 cyclohexylmethyl 4-nitrophenyl carbonate
  参考文献：
  名称：

  通过混合碳酸盐的新型分子内脱羧糖基化

  摘要：

  已经开发出两步糖基化方法，其涉及（1）通过使用碳酸盐作为连接物来连接两个糖，（2）借助于路易斯酸去除二氧化碳以形成糖苷键。该糖基化过程基于相反的连接方式，其中糖基受体被激活以连接糖。

  DOI：

  10.1016/0040-4039(96)00272-9

文献信息

• PIPERAZINES AS ANTI-OBESITY AGENTS
  申请人：Boyd Joseph W.

  公开号：US20110059969A1

  公开（公告）日：2011-03-10

  The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.

  本发明涉及公式（I）的新化合物，包括这些化合物的制药组合物，它们的制备过程，以及这些化合物作为瘦素受体调节剂类似物在制备用于治疗与体重增加、2型糖尿病和脂质代谢异常相关的疾病的药物中的用途。
• Use of 2, 4diamino-3-hydroxycarboxylic acid derivatives as proteasome inhibitors
  申请人：France Dennis

  公开号：US20050026994A1

  公开（公告）日：2005-02-03

  The present invention relates to the new use of 2,4-diamino-3-hydroxycarboxylic acids of formula (I), in which A and B independently represent a bond or an unsubstituted or substituted amino acyl moiety; R 1 represents hydrogen; an amino protecting group; or a group of formula R 5 Y— wherein R 5 represents hydrogen or an unsubstituted or substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y represents —CO—; —NH—CO—; —NH—CS—; —SO 2 —; —O—CO—; or —O—CS—; R 2 represents the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R 3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; and R 4 represents 2(R)-hydroxyindan-1(S)-yl; (S)-2-hydroxy-1-phenylethyl; or 2-hydroxy-benzyl unsubstituted or substituted in 4-position by methoxy; in the manufacture of a pharmaceutical composition for the treatment of a proliferative disease, e.g., of a solid tumor; to a method of treatment of warm-blooded animals; and to 2,4-diamino-3-hydroxycarboxylic acids of formula (I*), wherein A and B independently represent an unsubstituted or substituted amino acyl moiety; R 2 represents arylalkyl; R 3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; R 4 represents 2-hydroxy-benzyl unsubstituted or substituted in 4 position by methoxy; and R 5 represents arylalkyl and Y represents —CO—; or R 5 represents alkyl substituted by cycloalkyl, naphthyl, pyridyl or phenyl in which phenyl is substituted by alkyl or amino; and Y represents —O—CO; pharmaceutically acceptable salts thereof; and the use of such compounds of formula (I*) for the therapeutic treatment of the human or animal body, especially the treatment of proliferative diseases.

  本发明涉及式（I）的 2,4-二氨基-3-羟基羧酸的新用途，其中 A 和 B 独立地代表一个键或一个未取代或取代的氨基酰基；R 1 代表氢；氨基保护基；或式 R 5 Y- 其中 R 5 代表氢或未取代或取代的烷基、烯基、炔基、芳基、芳烷基、杂芳基、杂芳烷基、杂环烷基或杂环烷基；且 Y 代表 -CO-；-NH-CO-；-NH-CS-；-SO 2 -；-O-CO-；或-O-CS-； R 2 代表天然氨基酸的侧链；烷基、芳烷基、杂芳烷基或环烷基烷基；或三甲基硅甲基、2-噻吩甲基或苯乙烯甲基； R 3 3 代表卤素、烷基、烷氧基或羟基烷氧基；以及 R 4 代表 2(R)-羟基茚满-1(S)-基；(S)-2-羟基-1-苯基乙基；或未被甲氧基取代或在 4-位被甲氧基取代的 2-羟基苄基； 用于制造治疗增殖性疾病，例如式 (I*) 的 2,4-二氨基-3-羟基羧酸，其中 A 和 B 独立地代表未取代或取代的氨基酰基； R 2 代表芳烷基 3 代表卤素、烷基、烷氧基或羟基烷氧基； R 4 代表未取代的 2-羟基苄基或在 4 位被甲氧基取代的 2-羟基苄基；以及 R 5 代表芳烷基，Y 代表-CO-；或 R 5 代表被环烷基、萘基、吡啶基或苯基取代的烷基，其中苯基被烷基或氨基取代；且 Y 代表 -O-CO；其药学上可接受的盐；以及将式 (I*) 的此类化合物用于人体或动物机体的治疗，尤其是增殖性疾病的治疗。
• USE OF 2,4-DIAMINO-3-HYDROXYCARBOXYLIC ACID DERIVATIVES AS PROTEASOME INHIBITORS
  申请人：Novartis AG

  公开号：EP1173413B1

  公开（公告）日：2004-06-30
• [EN] USE OF 2,4-DIAMINO-3-HYDROXYCARBOXYLIC ACID DERIVATIVES AS PROTEASOME INHIBITORS<br/>[FR] DERIVES D'ACIDE 2,4-DIAMINO-3-HYDROXYCARBOXYLIQUE UTILISES COMME INHIBITEURS DE LA PROTEASOME
  申请人：NOVARTIS AG

  公开号：WO2000064863A1

  公开（公告）日：2000-11-02

  The present invention relates to the new use of 2,4-diamino-3-hydroxycarboxylic acids of formula (I), in which A and B independently represent a bond or an unsubstituted or substituted amino acyl moiety; R1 represents hydrogen; an amino protecting group; or a group of formula R5Y- wherein R5 represents hydrogen or an unsubstituted or substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y represents -CO-; -NH-CO-; -NH-CS-; -SO2-; -O-CO-; or -O-CS-; R2 represents the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; and R4 represents 2(R)-hydroxyindan-1(S)-yl; (S)-2-hydroxy-1-phenylethyl; or 2-hydroxy-benzyl unsubstituted or substituted in 4-position by methoxy; in the manufacture of a pharmaceutical composition for the treatment of a proliferative disease, e.g. of a solid tumor; to a method of treatment of warm-blooded animals; and to 2,4-diamino-3-hydroxycarboxylic acids of formula (I*), wherein A and B independently represent an unsubstituted or substituted amino acyl moiety; R2 represents arylalkyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; R4 represents 2-hydroxy-benzyl unsubstituted or substituted in 4 position by methoxy; and R5 represents arylalkyl and Y represents -CO-; or R5 represents alkyl substituted by cycloalkyl, naphthyl, pyridyl or phenyl in which phenyl is substituted by alkyl or amino; and Y represents -O-CO; pharmaceutically acceptable salts thereof; and the use of such compounds of formula (I*) for the therapeutic treatment of the human or animal body, especially the treatment of proliferative diseases.
• A novel intramolecular decarboxylative glycosylation via mixed carbonate
  作者：Takamasa Iimori、Takafumi Shibazaki、Shiro Ikegami

  DOI：10.1016/0040-4039(96)00272-9

  日期：1996.3

  A two-step glycosylation procedure, which involves (1) linking two sugars by using carbonate as a connector, (2) removing carbon dioxide to form a glycosidic bond by the aid of Lewis acid, has been developed. This glycosylation procedure was based on the opposite mode of connection, where a glycosyl acceptor was activated to link sugars.

  已经开发出两步糖基化方法，其涉及（1）通过使用碳酸盐作为连接物来连接两个糖，（2）借助于路易斯酸去除二氧化碳以形成糖苷键。该糖基化过程基于相反的连接方式，其中糖基受体被激活以连接糖。