(3R,4S)-1-tert-butoxycarbonyl-3,4-dihydroxypiperidine | 951766-53-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (3R,4S)-1-tert-butoxycarbonyl-3,4-dihydroxypiperidine
• 英文别名: tert-butyl (3R,4S)-3,4-dihydroxypiperidine-1-carboxylate；(3R,4S)-tert-Butyl 3,4-dihydroxypiperidine-1-carboxylate
• CAS: 951766-53-3
• 化学式: C₁₀H₁₉NO₄
• 分子量: 217.265
• InChiKey: RIZGRNBWPJMDKU-JGVFFNPUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  70
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (3R,4S)-1-tert-butoxycarbonyl-3,4-dihydroxypiperidine 在 potassium carbonate 作用下， 以 甲醇 、 二氯甲烷 、 水 为溶剂， 反应 3.0h， 生成 (3R,4S)-1-tert-butoxycarbonyl-3,4-epoxypiperidine
  参考文献：
  名称：

  2-Deoxyribose as a Rich Source of Chiral 5-Carbon Building Blocks

  摘要：

  [GRAPHICS]We have developed concise routes to a number of useful chiral 5-carbon synthetic building blocks using readily available: 0-1-methyl-2-deoxyribose as starting material. Novel transformations include the use of indium triflate to catalyze the oxidation of a methyl furanoside to the corresponding lactone with MCPBA and the Vasella-type fragmentation of a 5-iodo furanoside using chromium(II) chloride when zinc proved ineffective. In addition, 3,4-disubstitued piperidine derivatives were prepared without hydroxyl group protection via a simple reductive amination reaction.

  DOI：

  10.1021/jo0712143
• 作为产物：
  描述：

  甲基-2-脱氧-D-核糖 在 palladium on activated charcoal 吡啶 、 sodium azide 、 Amberlyst 15 、 氢气 、 四丁基碘化铵 作用下， 以 乙醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 20.0~80.0 ℃ 、413.7 kPa 条件下， 反应 112.0h， 生成 (3R,4S)-1-tert-butoxycarbonyl-3,4-dihydroxypiperidine
  参考文献：
  名称：

  2-Deoxyribose as a Rich Source of Chiral 5-Carbon Building Blocks

  摘要：

  [GRAPHICS]We have developed concise routes to a number of useful chiral 5-carbon synthetic building blocks using readily available: 0-1-methyl-2-deoxyribose as starting material. Novel transformations include the use of indium triflate to catalyze the oxidation of a methyl furanoside to the corresponding lactone with MCPBA and the Vasella-type fragmentation of a 5-iodo furanoside using chromium(II) chloride when zinc proved ineffective. In addition, 3,4-disubstitued piperidine derivatives were prepared without hydroxyl group protection via a simple reductive amination reaction.

  DOI：

  10.1021/jo0712143

文献信息

• [EN] PIPERIDINYLHYDROXYETHYLPIPERIDINES AS MODULATORS OF CHEMOKINE RECEPTORS<br/>[FR] PIPÉRIDINYLHYDROXYÉTHYLPIPÉRIDINES UTILISABLES EN TANT QUE MODULATEURS DES RÉCEPTEURS AUX CHIMIOKINES
  申请人：GLAXO GROUP LTD

  公开号：WO2009049113A1

  公开（公告）日：2009-04-16

  The present invention relates to a compound of the formula (I), or a pharmaceutically acceptable salt thereof, wherein R1-R8 and X, m, and n are defined. Compounds and compositions of the present invention are useful the treatment of atherosclerosis.

  本发明涉及公式（I）的化合物或其药学上可接受的盐，其中R1-R8和X、m和n已定义。本发明的化合物和组合物对动脉粥样硬化的治疗是有用的。
• DRUG COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING THROMBOSIS OR EMBOLISM
  申请人：OHTA Toshiharu

  公开号：US20090281074A1

  公开（公告）日：2009-11-12

  Drug compositions containing a substituted diamine compound represented by formula (1): Q 1 -Q 2 -r-N(R 1 )-Q 3 -N(R 2 )  (1) wherein Q 3 represents the following group wherein Q 5 represents an alkylene group having 4 carbon atoms, R 3 represents a hydrogen atom, and R 4 represents a 3-6 membered heterocyclic group which may be substituted; are useful for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after artificial valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

  含有以下式子（1）所代表的取代二胺化合物的药物组合物： Q1-Q2-r-N（R1）-Q3-N（R2）  （1） 其中，Q3代表以下基团： 其中，Q5代表具有4个碳原子的烷基基团，R3代表氢原子，R4代表可取代的3-6环杂环基团； 该药物组合物对于预防和/或治疗脑梗死、脑栓塞、心肌梗死、心绞痛、肺梗死、肺栓塞、布尔格病、深静脉血栓形成、弥散性血管内凝血综合征、人工瓣膜或关节置换后的血栓形成、血管成形术后的血栓形成和再闭塞、全身性炎症反应综合征（SIRS）、多器官功能障碍综合征（MODS）、体外循环期间的血栓形成或采血时的血凝。
• Diamine derivatives
  申请人：Ohta Toshiharu

  公开号：US20050119486A1

  公开（公告）日：2005-06-02

  A compound represented by the general formula (1): Q 1 -Q 2 -T 0 -N(R 1 )-Q 3 -N(R 2 )-T 1 -Q 4 (1) wherein R 1 and R 2 are hydrogen atoms or the like; Q 1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q 2 is a single bond or the like; Q 3 is a group in which Q 5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T 0 and T 1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

  一种由通式（1）表示的化合物：Q1-Q2-T0-N（R1）-Q3-N（R2）-T1-Q4（1），其中R1和R2是氢原子或类似物；Q1是饱和或不饱和的、5-或6-成员环烃基，可以被取代，或类似物；Q2是单键或类似物；Q3是其中Q5是具有1到8个碳原子的烷基，或类似物；T0和T1是羰基或类似物；其盐、溶剂化物或N-氧化物。该化合物可用作预防和/或治疗脑梗死、脑栓塞、心肌梗死、心绞痛、肺梗死、肺栓塞、布尔格病、深静脉血栓形成、弥散性血管内凝血综合症、瓣膜或关节置换后的血栓形成、血管成形术后的血栓形成和再闭塞、全身性炎症反应综合征（SIRS）、多器官功能障碍综合征（MODS）、体外循环期间的血栓形成或采血时的血液凝固。
• DIAMINE DERIVATIVES
  申请人：Ohta Toshiharu

  公开号：US20100093785A1

  公开（公告）日：2010-04-15

  A compound represented by the general formula (1): -Q 1 -Q 2 -T 0 -N(R 1 )-Q 3 -(R 2 )T 1 Q 4 (1) wherein R 1 and R 2 are hydrogen atoms or the like; Q 1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q 2 is a single bond or the like; Q 3 is a group in which Q 5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T 0 and T 1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

  一种化合物，其一般式（1）如下：-Q1-Q2-T0-N（R1）-Q3-（R2）T1Q4（1），其中R1和R2是氢原子或类似物；Q1是饱和或不饱和的5或6元环烃基，可能被取代，或类似物；Q2是单键或类似物；Q3是其中Q5是具有1至8个碳原子的烷基，或类似物的基团；T0和T1是羰基基团或类似物；其盐、溶剂化合物或N-氧化物。该化合物可用作预防和/或治疗脑梗死、脑栓塞、心肌梗死、心绞痛、肺梗死、肺栓塞、布尔格病、深静脉血栓形成、弥散性血管内凝血综合征、瓣膜或关节置换后的血栓形成、血管成形术后的血栓形成和再闭塞、全身性炎症反应综合征（SIRS）、多器官功能障碍综合征（MODS）、体外循环期间的血栓形成或采血时的血凝。
• NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS
  申请人：MANOHARAN Muthiah

  公开号：US20120095075A1

  公开（公告）日：2012-04-19

  The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

  本发明提供了有利于用于体内向细胞传递治疗剂的脂质。具体而言，本发明提供具有以下结构的脂质：