Phosphorsaeure-(p-chlorphenylester)-dichlorid

• 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: Phosphorsaeure-(p-chlorphenylester)-dichlorid
• 英文别名: Dichloro (4-chlorophenyl) phosphate
• 化学式: C₆H₄Cl₃O₄P
• 分子量: 277.428
• InChiKey: CLOSNUYMZFZPNI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  44.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  Phosphorsaeure-(p-chlorphenylester)-dichlorid 在 三乙胺 作用下， 以 吡啶 、 乙腈 为溶剂， 反应 1.08h， 生成 4-chlorophenyl 5'-O-(4,4'-dimethoxytrityl)-N⁶-benzoyl-2'-deoxyadenosin-3'-yl phosphate triethylammonium salt
  参考文献：
  名称：

  Michels, Winfried; Schlimme, Eckhard, Liebigs Annalen der Chemie, 1982, # 7, p. 1398 - 1402

  摘要：

  DOI：

文献信息

• Process for the preparation of cytidine derivatives
  申请人：——

  公开号：US20030032797A1

  公开（公告）日：2003-02-13

  An efficient method for producing cytidine derivatives that took away the previous drawbacks by efficiently synthesizing cytidine derivatives by utilizing a tertiary amine can be provided.

  一种高效生产胞嘧啶衍生物的方法，通过利用三级胺有效地合成胞嘧啶衍生物，从而消除了先前的缺点。
• Anti-HCV nucleoside derivatives
  申请人：——

  公开号：US20030008841A1

  公开（公告）日：2003-01-09

  The present invention comprises novel and known purine and pyrimidine nucleoside derivatives which have been discovered to be active against hepatitis C virus (HCV). The use of these derivatives for the treatment of HCV infection is claimed as are the novel nucleoside derivatives disclosed herein.

  本发明涉及新颖和已知的嘌呤和嘧啶核苷衍生物，已发现这些衍生物对丙型肝炎病毒（HCV）具有活性。本发明声明利用这些衍生物治疗HCV感染，以及本文所披露的新颖核苷衍生物。
• [EN] NOVEL PRODRUGS OF MIZORIBINE<br/>[FR] NOUVEAUX PROMÉDICAMENTS DE MIZORIBINE
  申请人：UNIV LEUVEN KATH

  公开号：WO2018134399A1

  公开（公告）日：2018-07-26

  The present invention relates to novel prodrugs of mizoribine, and a method for their preparation, as well as to pharmaceutical compositions comprising these prodrugs and one or more pharmaceutically acceptable excipients. The present invention further relates to the use of said novel prodrugs as biologically active ingredients, specifically in combination with other biologically active drugs such as immunosuppressants and/or immunomodulatory drugs, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and autoimmune disorders, organ and cells transplant rejection.

  本发明涉及美津利宾的新型前药，以及其制备方法，以及包含这些前药和一个或多个药学上可接受的赋形剂的药物组合物。本发明进一步涉及将这些新型前药用作生物活性成分，特别是与其他生物活性药物（如免疫抑制剂和/或免疫调节药物）结合使用，更具体地作为治疗疾病和病理病况的药物，如但不限于免疫和自身免疫性疾病，器官和细胞移植排斥等。
• [EN] PROCESSES FOR PREPARING 4'AZIDO NUCLEOSIDE DERIVATIVES<br/>[FR] METHODES DE PREPARATION DE DERIVES DE 4'AZIDO NUCLEOSIDE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2005000864A1

  公开（公告）日：2005-01-06

  A process for the preparation of a 4’-azido-2’,3’,5’-triacyl-nucleoside compound (I;B=B1; R1 is R1aCO-and R2 is R2aCO-) or a 4’-azidonucleoside compounds (I; B is B1 or B2 and R1 and R2 are hydrogen and acid addition salts thereof) wherein R1a and R2a are independently C1-10 alkyl or phenyl optionally substituted with 1 to 3 substituents selected from the group consisting of alkyl, alkoxy, halogen, nitro or cyano and R3 is selected from the group consisting of hydrogen, C1-6 alkyl, C1-3 haloalkyl and halogen, comprising contacting a 5’-iodo compound II with a peracid, R2aC(O)OOH, an acid R2aC(O)OH and a phase transfer catalyst and interconverting a uridine B1 to a cytosine B2. The present process provides the 4’-azidonucleosides safely and selectively in high purity with increased efficiency.

  一种制备4'-偶氮-2'，3'，5'-三酰基-核苷化合物（I；B=B1；R1为R1aCO-，R2为R2aCO-）或4'-偶氮核苷化合物（I；B为B1或B2，R1和R2为氢及其酸盐）的方法，其中R1a和R2a独立地为C1-10烷基或苯基，可选地取代为1至3个来自烷基、烷氧基、卤素、硝基或氰基的取代基，R3选自氢、C1-6烷基、C1-3卤代烷基和卤素组成，包括将5'-碘化合物II与过氧酸、R2aC（O）OOH、酸R2aC（O）OH和相转移催化剂接触，将尿苷B1互变为胞嘧啶B2。该过程以提高效率安全、选择性地提供高纯度的4'-偶氮核苷化合物。
• [EN] 2,3'-Anhydro-2'-deoxy-5-fluorouridine derivatives with cytotoxic activity, a manufacturing process and application<br/>[FR] DÉRIVÉS DE 2,3'-ANHYDRO-2'-DÉSOXY-5-FLUOROURIDINE À ACTIVITÉ CYTOTOXIQUE, PROCÉDÉ DE FABRICATION ET APPLICATION
  申请人：UNIV ADAM MICKIEWICZ

  公开号：WO2015050468A1

  公开（公告）日：2015-04-09

  The subject matter of the invention is novel 2,3'-anhydro-2'-deoxy-5-fluorouridine derivatives of general formula (1) where R is a trifluoromethyl, 2,2,2-trifluoroethyl, difluoromethyl, perfluoroethyl, 1-fluoroethyl, 2-fluoroethyl, 1,1-difluoroethyl, 1,2-difluoroethyl, 2,2-difluoroethyl, 1,1,2-trifluoroethyl, 1,2,2-trifluoroethyl, 1,1,2,2-tetrafluoroethyl, 1,2,2,2-tetrafluoroethyl group. In a second aspect, the subject matter of the invention is a process for the manufacture of 2,3'-anhydro-2'-deoxy-5-fluorouridine derivatives of general formula (1). In a third aspect, the subject matter of the invention is an application of 2,3'-anhydro-2'-deoxy-5-fluorouridine derivatives of general formula (1) in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

  本发明涉及通式（1）中R为三氟甲基、2,2,2-三氟乙基、二氟甲基、全氟乙基、1-氟乙基、2-氟乙基、1,1-二氟乙基、1,2-二氟乙基、2,2-二氟乙基、1,1,2-三氟乙基、1,2,2-三氟乙基、1,1,2,2-四氟乙基、1,2,2,2-四氟乙基基团的新型2,3'-去氧-2'-脱氧-5-氟尿苷衍生物的主题。其次，本发明涉及一种制备通式（1）中2,3'-去氧-2'-脱氧-5-氟尿苷衍生物的方法。第三，本发明涉及通式（1）中2,3'-去氧-2'-脱氧-5-氟尿苷衍生物在乳腺癌、宫颈癌、肺癌和鼻咽癌的抗癌治疗中的应用。