p-Nitrophenyl phosphinate | 53204-64-1

• 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: p-Nitrophenyl phosphinate
• 英文别名: 1-nitro-4-phosphorosooxybenzene
• CAS: 53204-64-1
• 化学式: C6H4NO4P
• 分子量: 185.07
• InChiKey: RPLNFVZIGAYKDT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  72.1
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] DIASTEREOSELECTIVE SYNTHESIS OF PHOSPHATE DERIVATIVES AND OF THE GEMCITABINE PRODRUG NUC-1031<br/>[FR] SYNTHÈSE DIASTÉRÉOSÉLECTIVE DE DÉRIVÉS DE PHOSPHATE ET DU PROMÉDICAMENT DE GEMCITABINE NUC-1031
  申请人：NUCANA BIOMED LTD

  公开号：WO2017098252A1

  公开（公告）日：2017-06-15

  The present invention provides a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. It also provides a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate.

  本发明提供了一种用于合成吉西他滨-[苯基苯氧基-L-丙氨酰)]-磷酸盐中间体的制备方法。它还提供了一种制备吉西他滨-[苯基苯氧基-L-丙氨酰)]-磷酸盐的方法。
• [EN] N- [ (2 ' R) -2 ' -DEOXY-2 ' -FLUORO-2 ' -METHYL-P-PHENYL-5 ' -URIDYLYL] -L-ALANINE 1-METHYLETHYL ESTER AND PROCESS FOR ITS PRODUCTION<br/>[FR] ESTER DE N-[(2 ' R) -2' -DÉSOXY-2' -FLUORO-2' -MÉTHYL-P-PHÉNYL-5' -URIDYLYL]-L-ALANINE 1-MÉTHYLÉTHYLE ET SON PROCÉDÉ DE PRODUCTION
  申请人：PHARMASSET INC

  公开号：WO2010135569A1

  公开（公告）日：2010-11-25

  Disclosed herein are nucleoside phosphoramidates of formula 4 and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals. Disclosed is also a process for preparing compound represented by formula 4: (Formula 4) wherein P* represents a chiral phosphorus atom, which comprises: a) reacting an isopropyl-alanate, (Formula A), a di-X'-phenylphosphate, (Formula B), 2'-deoxy-2f-fluoro-2'-C-methyluridine, (Formula 3), and a base to obtain a first mixture comprising 4; wherein X is a conjugate base of an acid, n is 0 or 1, and X' is a halogen, b) reacting the first mixture with a protecting compound to obtain a second mixture comprising 4; and c) optionally subjecting the second mixture to crystallization, chromatography or extraction in order to obtain 4.

  本文披露了化学式4的核苷酸磷酰胺及其作为治疗病毒性疾病的药物的用途。这些化合物是RNA依赖性5RNA病毒复制的抑制剂，可作为HCV NS5B聚合酶的抑制剂，HCV复制的抑制剂以及哺乳动物丙型肝炎感染的治疗药物。还披露了一种制备化合物4的方法：（化学式4），其中P*代表手性磷原子，包括：a）反应异丙基-丙氨酸酯（化学式A）、二-X'-苯基磷酸酯（化学式B）、2'-脱氧-2f-氟-2'-C-甲基尿嘧啶（化学式3）和碱以获得含有4的第一混合物；其中X是酸的共轭碱基，n为0或1，X'是卤素；b）将第一混合物与保护化合物反应以获得含有4的第二混合物；c）可选地将第二混合物经结晶、色谱或萃取处理以获得4。
• [EN] PROCESS FOR THE PREPARATION OF SOFOSBUVIR<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION DE SOFOSBUVIR
  申请人：HC-PHARMA AG

  公开号：WO2017144423A1

  公开（公告）日：2017-08-31

  The present invention relates to a process for the synthesis of Sofosbuvir of formula (I) comprising the selective mono-deacetylation reaction of a compound of formula (V) to obtain a compound of formula (IV).

  本发明涉及一种用于合成式（I）的索非布韦的过程，包括选择性单去乙酰化反应化合物式（V）以获得化合物式（IV）。
• NUCLEOSIDE PHOSPHORAMIDATES
  申请人：Ross Bruce S.

  公开号：US20110251152A1

  公开（公告）日：2011-10-13

  Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

  本文披露了核苷酸磷酰胺及其作为治疗病毒性疾病的药物的用途。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用作HCV NS5B聚合酶的抑制剂，用于抑制HCV复制并治疗哺乳动物的丙型肝炎感染。
• Stereoselective synthesis of phosphorus containing actives
  申请人：Gilead Pharmasset LLC

  公开号：EP2752422B1

  公开（公告）日：2017-08-16