N-(1,2-oxazol-3-yl)benzenesulfonamide | 900415-31-8

• 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: N-(1,2-oxazol-3-yl)benzenesulfonamide
• CAS: 900415-31-8
• 化学式: C₉H₈N₂O₃S
• mdl: MFCD05099850
• 分子量: 224.24
• InChiKey: NRNITHABNQZDAT-UHFFFAOYSA-N

物化性质

• 沸点：
  410.4±37.0 °C(Predicted)
• 密度：
  1.450±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  80.6
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] METHOD FOR THE PREPARATION OF DIARYLISOXAZOLE SULFONAMIDE COMPOUNDS AND INTERMEDIATES<br/>[FR] PROCEDES DESTINES LA PREPARATION D'UN COMPOSE DE DIARYLISOXAZOLE SULFONAMIDE ET D'INTERMEDIAIRES
  申请人：PHARMACIA CORP

  公开号：WO2005123701A1

  公开（公告）日：2005-12-29

  The disclosure provides a method for the preparation of a diarylisoxazolé sulfonamide compound comprising contacting a deoxybenzoin with a secondary amine to form a diarylenamine compound; contacting the diarylenamine compound with an acetylating agent to form an acetyl diarylenamine compound; contacting the acetyl diarylenamine compound with a source of hydroxylamine to form an diaryl isoxazolol compound; eliminating water from the diaryl isoxazolol compound to form a diaryl isoxazole compound, chlorosulfonating the diarylisoxazole compound to form a chlorosulfonyl diaryl isoxazole compound; and contacting the chlorosulfonyl diaryl isoxazole compound with a source of ammonia to form the diarylisoxazole sulfonamide compound.

  该公开提供了一种制备二芳基异噁唑磺胺化合物的方法，包括将脱氧苯并与二级胺接触以形成二芳胺化合物；将二芳胺化合物与乙酰化剂接触以形成乙酰二芳胺化合物；将乙酰二芳胺化合物与羟胺源接触以形成二芳异噁唑醇化合物；从二芳异噁唑醇化合物中除去水分以形成二芳异噁唑化合物，将二芳异噁唑化合物氯磺化以形成氯磺基二芳异噁唑化合物；并将氯磺基二芳异噁唑化合物与氨源接触以形成二芳异噁唑磺胺化合物。
• [EN] NEUTRAL ENDOPEPTIDASE INHIBITOR POLYMORPH<br/>[FR] POLYMORPHE INHIBITEUR D'ENDOPEPTIDASE NEUTRE
  申请人：PFIZER LTD

  公开号：WO2005123702A1

  公开（公告）日：2005-12-29

  Disclosed are (2S)-2-1-[(1S)-1-Isobutoxycarbonyl-2-(5-phenyl-oxazol-2-yl)-ethylcarbamoyl]-cyclopentylmethyl}-4-methoxy-butyric, Potassium-(2S)-2-1-[(1S)-1-Isobutoxycarbonyl-2-(5-phenyl-oxazol-2-yl)-ethylcarbamoyl]-cyclopentylmethyl}-4-methoxy-butyrate, monohydrate and its Form I polymorph. Also disclosed are compositions of the described forms, kits including the described forms, and methods of using the described forms for the treatment diseases or disorders where the use of a neutral endopeptidase inhibitor is indicated, including cardiovascular diseases and conditions.

  披露了(2S)-2-1-[(1S)-1-异丁氧羰基-2-(5-苯基-噁唑-2-基)-乙基氨基]-环戊甲基}-4-甲氧基丁酸钾盐、(2S)-2-1-[(1S)-1-异丁氧羰基-2-(5-苯基-噁唑-2-基)-乙基氨基]-环戊甲基}-4-甲氧基丁酸盐、单水合物及其I型多形体。还披露了所述形式的组合物、包含所述形式的试剂盒，以及使用所述形式治疗心血管疾病和症状等需要使用中性内肽酶抑制剂的疾病或疾病的方法。
• Method for preparing benzenesulfonyl compounds
  申请人：——

  公开号：US20030105334A1

  公开（公告）日：2003-06-05

  The present disclosure provides a method for the preparation of aromatic sulfonyl halides by contacting a substituted phenyl compound with a halosulfonic acid and trifluoroacetic acid. The present disclosure further provides a method for the preparation of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide which is useful in treating cyclooxygenase-2 related disorders.

  本公开提供了一种制备芳香基磺酰卤化物的方法，该方法是通过将取代苯基化合物与卤代磺酸和三氟乙酸接触来实现的。本公开还提供了一种制备4-［5-甲基-3-苯基异噁唑-4-基］苯磺酰胺的方法，该方法可用于治疗环氧合酶-2相关疾病。
• Sulfonamides and derivatives thereof that modulate the activity of endothelin
  申请人：Texas Biotechnology Corporation

  公开号：US20010056183A1

  公开（公告）日：2001-12-27

  Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazolyl)phenylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.

  提供了噻吩基、呋喃基、吡咯基和苯基磺酰胺，以及其药学上可接受的衍生物的配方和调节或改变内皮素家族肽活性的方法。具体而言，提供了N-(异噁唑基)噻吩基磺酰胺、N-(异噁唑基)呋喃基磺酰胺、N-(异噁唑基)吡咯基磺酰胺和N-(异噁唑基)苯基磺酰胺，以及这些磺酰胺的配方和使用这些磺酰胺通过与受体接触来抑制内皮素肽与内皮素受体的结合的方法。还提供了通过给予这些磺酰胺或药学上可接受的抑制内皮素活性的衍生物的有效量来治疗内皮素介导的疾病的方法。
• [EN] METHOD FOR PREPARING BENZENESULFONYL COMPOUNDS<br/>[FR] PROCEDE DE PREPARATION DE COMPOSES DE BENZENESULFONYLE
  申请人：PHARMACIA CORP

  公开号：WO2003029230A1

  公开（公告）日：2003-04-10

  The present disclosure provides a method for the preparation of aromatic sulfonyl halides by contacting a substituted phenyl compound with a halosulfonic acid and trifluoroacetic acid. The present disclosure further provides a method for the preparation of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide which is useful in treating cyclooxygenase-2 related disorders.

  本公开提供了一种制备芳基磺酰卤化物的方法，其中通过将取代苯基化合物与卤代磺酸和三氟乙酸接触。本公开还提供了一种制备4-[5-甲基-3-苯基异噁唑-4-基]苯磺酰胺的方法，该方法在治疗环氧合酶-2相关疾病方面有用。