(1R,2R)-1-(chloroamino)-2-(difluoromethyl)-N-(1-methylcyclopropyl)sulfonylcyclopropane-1-carboxamide

• 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: (1R,2R)-1-(chloroamino)-2-(difluoromethyl)-N-(1-methylcyclopropyl)sulfonylcyclopropane-1-carboxamide
• 化学式: C₉H₁₃ClF₂N₂O₃S
• 分子量: 302.73
• InChiKey: BMPGYAXSCUOWCA-SSDLBLMSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  83.6
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• SYNTHESIS OF AN ANTIVIRAL COMPOUND
  申请人：Cagulada Amy

  公开号：US20150175626A1

  公开（公告）日：2015-06-25

  The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

  本公开提供了一种制备式I化合物的方法，该化合物可用作抗病毒剂。本公开还提供了用于制备化合物的方法和化合物，这些化合物是式I化合物的合成中间体。
• CRYSTALLINE FORMS OF AN ANTIVIRAL COMPOUND
  申请人：GILEAD SCIENCES, INC.

  公开号：US20150175625A1

  公开（公告）日：2015-06-25

  Crystalline forms of the anti-HCV compound (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.

  抗丙型肝炎化合物的结晶形式（1aR,5S,8S,9S,10R,22aR）-5-叔丁基-N-[(1R,2R)-2-(二氟甲基)-1-[(1-甲基环丙基)磺酰胺基]羰基}环丙基]-9-乙基-18,18-二氟-14-甲氧基-3,6-二氧基-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-十四氢-8H-7,10-甲基环丙[18,19][1,10,3,6]二氧杂环戊二烯[11,12-b]喹诺沙啉-8-羧酰胺（化合物I）已在固态中制备和表征：同时提供了制造过程和使用结晶形式的方法。
• MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS
  申请人：Enanta Pharmaceuticals, Inc.

  公开号：US20140194350A1

  公开（公告）日：2014-07-10

  The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

  本发明披露了I式化合物或其药学上可接受的盐、酯或前药：其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。因此，本发明的化合物干扰了丙型肝炎病毒的生命周期，也可用作抗病毒剂。本发明还涉及包含上述化合物的制药组合物，用于治疗患有HCV感染的受试者。本发明还涉及通过给予包含本发明化合物的制药组合物来治疗受试者的HCV感染的方法。
• [EN] SYNTHESIS OF A MACROCYCLIC HCV NS3 INHIBITING TRIPEPTIDE<br/>[FR] SYNTHÈSE D'UN TRIPEPTIDE INHIBANT LE NS3 DU VIRUS DE L'HÉPATITE C MACROCYCLIQUE
  申请人：GILEAD SCIENCES INC

  公开号：WO2015100145A1

  公开（公告）日：2015-07-02

  The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

  本公开提供了制备式I化合物的过程，该化合物可用作抗病毒剂。该公开还提供了化合物及制备该化合物的过程，该化合物是式I化合物的合成中间体。
• Synthesis of an antiviral compound
  申请人：Gilead Sciences, Inc.

  公开号：US10030033B2

  公开（公告）日：2018-07-24

  The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

  本公开提供了用作抗病毒剂的式Ⅰ化合物的制备工艺。 本公开还提供了作为式 I 化合物合成中间体的化合物及其制备工艺。