1-(苯基磺酰基)哌啶-3-醇 | 1021372-74-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 1-(苯基磺酰基)哌啶-3-醇
• 英文名称: 1-(phenylsulfonyl)piperidin-3-ol
• 英文别名: 1-(Benzenesulfonyl)piperidin-3-ol
• CAS: 1021372-74-6
• 化学式: C₁₁H₁₅NO₃S
• mdl: MFCD12179656
• 分子量: 241.311
• InChiKey: RSERXZKOBVKAOP-UHFFFAOYSA-N

物化性质

• 沸点：
  410.7±55.0 °C(Predicted)
• 密度：
  1.327±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.454
• 拓扑面积：
  66
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(苯基磺酰基)哌啶-3-醇 在 pyridinium chlorochromate 作用下， 以 二氯甲烷 为溶剂， 生成 1-苯磺酰基-3-哌啶酮
  参考文献：
  名称：

  Synthesis of 1,2,4-trisubstituted-1,2,5,6-tetrahydropyridines

  摘要：

  A novel method for the synthesis of 1,2,4-trisubstituted- or 1,2,3,4-tetrasubstituted-1,2,5,6-tetrahydropyridine is presented. The process was carried out by the bromomethoxylation of 4-substituted-1,2,5,6-tetrahydropyridines 1 with N-bromosuccinimide (NBS) in methanol, dehydrobromination with 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), and boron trifluoride etherate (BF(3)-OEt(2))-catalyzed cross coupling of the corresponding enamine with trimethylsilyl-based nucleophiles. Homokainoid analogs were also synthesized via the protocol. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2010.11.131
• 作为产物：
  描述：

  3-羟基哌啶 、 苯磺酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 5.0h， 以99%的产率得到1-(苯基磺酰基)哌啶-3-醇
  参考文献：
  名称：

  Synthesis of rodocaine

  摘要：

  A new method for synthesis of rodocaine (1) is presented. Two key steps were carried out by the N-bromosuccinimide (NBS)-mediated intermolecular addition of known enamine 5 with allyltrimethyl silane in presence of boron trifluoride etherate (BF3/OEt2) and the intramolecular ring-closing metathesis of triene 3. The Diels-Alder cycloaddition of triene 3 with different ethyl propiolates was also studied. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2011.08.025

文献信息

• [EN] FUSED BICYCLIC COMPOUNDS AND USE THEREOF AS PI3K INHIBITORS<br/>[FR] COMPOSÉS BICYCLIQUES FUSIONNÉS ET UTILISATIONS DE CEUX-CI COMME INHIBITEURS DE P13K
  申请人：MERCK SERONO SA

  公开号：WO2009133127A1

  公开（公告）日：2009-11-05

  The invention relates to compounds of formula (I), for the regulation of phosphoinositides 3-kinases activity and related diseases.

  这项发明涉及到式(I)的化合物，用于调节磷脂酰肌醇3-激酶的活性和相关疾病。
• [EN] FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE<br/>[FR] COMPOSÉS BICYCLIQUES FUSIONNÉS UTILISÉS COMME INHIBITEURS DE LA PI3 KINASE
  申请人：MERCK SERONO SA

  公开号：WO2010100144A1

  公开（公告）日：2010-09-10

  The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.

  该发明涉及用于调节磷脂酰肌醇3-激酶活性及相关疾病的化合物（I）的公式。
• Metal-free synthesis of sulfonamides via iodine-catalyzed oxidative coupling of sulfonyl hydrazides and amines
  作者：Santosh Kumar Reddy Parumala、Rama Krishna Peddinti

  DOI：10.1016/j.tetlet.2016.02.009

  日期：2016.3

  A novel, rapid, and environmentally-friendly protocol for the synthesis of sulfonamides using iodine as catalyst under solvent-free conditions is described. This method involves the oxidative coupling of sulfonyl hydrazides and amines in the presence of catalytic amount of iodine using TBHP as oxidant. This protocol does not require purification techniques such as column chromatography and recrystalization

  描述了一种在无溶剂条件下使用碘作为催化剂合成磺酰胺的新颖，快速且环境友好的方案。该方法涉及在使用TBHP作为氧化剂的催化量碘存在下，磺酰肼和胺的氧化偶联。该方案不需要纯化技术，例如柱色谱法和重结晶法。
• INHIBITORS OF CYSTEINE PROTEASE
  申请人：SMITHKLINE BEECHAM CORPORATION

  公开号：EP0936912A1

  公开（公告）日：1999-08-25
• EP0936912A4
  申请人：——

  公开号：EP0936912A4

  公开（公告）日：1999-10-13