2-Nitro-4-phenylsulfinyl-chlorbenzol | 92114-67-5

• 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: 2-Nitro-4-phenylsulfinyl-chlorbenzol
• 英文别名: phenyl-(4-chloro-3-nitrophenyl) sulfoxide；4-(benzenesulfinyl)-1-chloro-2-nitrobenzene
• CAS: 92114-67-5
• 化学式: C₁₂H₈ClNO₃S
• 分子量: 281.719
• InChiKey: LIQQYWQEWFGIIR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  82.1
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-Nitro-4-phenylsulfinyl-chlorbenzol 在 氨 、 三氯化磷 作用下， 以 甲醇 、 氯仿 为溶剂， 反应 11.0h， 生成 2-nitro-4-phenylthioaniline
  参考文献：
  名称：

  Wollweber; Kolling; Niemers, Arzneimittel-Forschung/Drug Research, 1984, vol. 34, # 5, p. 531 - 542

  摘要：

  DOI：
• 作为产物：
  描述：

  3-硝基-4-氯苯胺 在 盐酸 、 sodium hydroxide 、 双氧水 、 铜 、 sodium nitrite 作用下， 以 乙酸酐 为溶剂， 反应 49.0h， 生成 2-Nitro-4-phenylsulfinyl-chlorbenzol
  参考文献：
  名称：

  Wollweber; Kolling; Niemers, Arzneimittel-Forschung/Drug Research, 1984, vol. 34, # 5, p. 531 - 542

  摘要：

  DOI：

文献信息

• Nitrodiaryl sulfoxide derivatives, process for their preparation and
  申请人：Richter Gedeon Vegyeszeti Gyar Rt

  公开号：US04710323A1

  公开（公告）日：1987-12-01

  The invention relates to a new process for the preparation of aminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein X is halogen, alkoxy having from 1 to 6 carbon atoms or a group --(N,R,R.sup.1), in which R and R.sup.1 are hydrogen or alkyl having from 1 to 6 carbon atoms, R.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or phenyl or phenylthio both optionally substituted by one or more identical or different halogen(s) and/or amino group(s), and acid addition salts thereof. The compounds of formula (I) are pharmaceutically active, in particular are potent anthelmintics, or can be used as active ingredients in pesticidal compositions. The invention therefore relates to pharmaceutical and pesticidal compositions containing compounds of formula (I) or salts thereof as active ingredient. Compounds of formula (I), in which the substituents are as defined above, but if X stands for a group --N(R,R.sup.1) in which R and R.sup.1 both represent hydrogen, and X is in para-position related to the sulfoxide group, then R.sup.2 is other than hydrogen, halogen, alkyl having from 1 to 6 carbon atoms and alkoxy having from 1 to 6 carbon atoms, and the acid addition salts thereof, are new. These new compounds are also subject of the present invention.

  该发明涉及一种新的制备氨基二芳基亚砜衍生物的方法，其化学式为(I)， 其中X为卤素、含有1至6个碳原子的烷氧基或一个基团--(N,R,R1)，其中R和R1为氢或含有1至6个碳原子的烷基，R2为氢、卤素、含有1至6个碳原子的烷基、含有1至6个碳原子的烷氧基或苯基或苯硫基，两者可以选择性地被一个或多个相同或不同的卤素和/或氨基取代，以及它们的酸盐。化合物的化学式(I)具有药理活性，特别是作为强效驱虫剂，或可用作杀虫剂组合物中的活性成分。因此，该发明涉及含有化合物的药物和杀虫剂组合物的制备方法(I)或其酸盐作为活性成分。化合物的化学式(I)中，取代基如上所定义，但如果X代表一个基团--N(R,R1)，其中R和R1均表示氢，并且X与亚砜基相关联在对位，则R2不是氢、卤素、含有1至6个碳原子的烷基和含有1至6个碳原子的烷氧基，其酸盐，均为新化合物。这些新化合物也是本发明的主题。
• Nitraminodiaryl sulfoxide derivatives, process for their preparation and
  申请人：Richter Gedeon Vegyeszeti Gyor Rt.

  公开号：US04956007A1

  公开（公告）日：1990-09-11

  The invention relates to a new process for the preparation of nitraminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein R and R.sup.1 represent hydrogen or alkyl having from 1 to 6 carbon atoms, and R.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms, or phenyl or thiophenyl both optionally substituted by one or more identical or different halogen(s) and/or nitro group(s). The compounds of formula (I) are pharmaceutically active, and are particularly useful in the veterinary therapy as anthelmintics. In addition they show pesticidal, particularly acaricidal, fungicidal and herbicidal properties. The invention relates also to pharmaceutical and pesticidal compositions containing as active ingredient compounds of formula (I). The compounds of formula (I), in which the substituents are as defined, with the proviso that if R.sup.2 is hydrogen and the substituent --N(R,R.sup.1) is in para-position related to the sulfoxide group, R and R.sup.1 are other than hydrogen or methyl, are new.

  本发明涉及一种新的制备硝基氨基二芳基亚砜衍生物的方法，其化学式为（I）：##STR1## 其中R和R.sup.1代表氢或具有1至6个碳原子的烷基，R.sup.2为氢、卤素、具有1至6个碳原子的烷基、具有1至6个碳原子的烷氧基、苯基或噻吩基，这些基团都可以选择性地被一个或多个相同或不同的卤素和/或硝基取代。化合物（I）具有药理活性，特别适用于兽医治疗作为驱虫剂。此外，它们还表现出杀虫、特别是杀螨、杀真菌和除草的性质。本发明还涉及含有化合物（I）作为活性成分的药物和杀虫剂组合物。化合物（I）中，如果R.sup.2为氢且取代基--N(R,R.sup.1)与亚砜基相对位于对位，则R和R.sup.1不是氢或甲基，则为新化合物。
• Aminodiaryl sulfoxide derivatives, process for their preparation and
  申请人：Richter Gedeon Vegyeszeti Gyar Rt

  公开号：US04985463A1

  公开（公告）日：1991-01-15

  An antifungal or anthelmintic method of treatment is disclosed which comprises the step of administering to a mammal in need of said treatment, a pharmaceutically effective amount of a compound of the Formula (I) ##STR1## wherein X is halogen, C.sub.1 to C.sub.6 alkoxy, or a group --NRR.sup.1 in which R and R.sup.1 are each hydrogen or C.sub.1 to C.sub.6 alkyl; and R.sup.2 is hydrogen, halogen, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, phenyl, phenylthio, or phenyl or phenylthio substituted by at least one halogen or amino substituent; or a pharmaceutically acceptable acid addition salt thereof.

  本发明公开了一种抗真菌或抗寄生虫的治疗方法，其包括向需要该治疗的哺乳动物施用化学药物有效量的化合物（I）：##STR1##其中X是卤素，C.sub.1至C.sub.6烷氧基或--NRR.sup.1基团，其中R和R.sup.1均为氢或C.sub.1至C.sub.6烷基；R.sup.2是氢、卤素、C.sub.1至C.sub.6烷基、C.sub.1至C.sub.6烷氧基、苯基、苯硫基或至少有一个卤素或氨基取代的苯基或苯硫基；或其药学上可接受的酸加盐。
• Process for the preparation of nitrodiaryl sulfoxides
  申请人：Richter Gedeon Vegyeszeti Gyar Rt.

  公开号：US04831194A1

  公开（公告）日：1989-05-16

  The invention relates to a new process for the preparation of aminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein X is halogen, alkoxy having from 1 to 6 carbon atoms or a group --(N,R,R.sup.1), in which p1 R and R.sup.1 are hydrogen or alkyl having from 1 to 6 carbon atoms, R.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or phenyl or phenylthio both optionally substituted by one or more identical or different halogen(s) and/or amino group(s), and acid addition salts thereof. The compounds of formula (I) are pharmaceutically active, in particular are potent anthelmintics, or can be used as active ingredients in pesticidal compositions. The invention therefore relates to pharmaceutical and pesticidal compositions containing compounds of formula (I) or salts thereof as active ingredient. Compounds of formula (I), in which the substituents are as defined above, but if X stands for a group --N(R,R.sup.1) in which R and R.sup.1 both represent hydrogen, and X is in para-position related to the sulfoxide group, then R.sup.2 is other than hydrogen, halogen, alkyl having from 1 to 6 carbon atoms and alkoxy having from 1 to 6 carbon atoms, and the acid addition salts thereof, are new. These new compounds are also subject of the present invention.

  本发明涉及一种制备公式（I）的氨基二芳基亚砜衍生物的新工艺，其中X为卤素，具有1至6个碳原子的烷氧基或基团--（N，R，R1），其中p1 R和R1均为氢或具有1至6个碳原子的烷基，R2为氢、卤素、具有1至6个碳原子的烷基、具有1至6个碳原子的烷氧基或苯基或苯硫基，两者都可以选择地被一个或多个相同或不同的卤素和/或氨基替代，以及它们的酸加成盐。公式（I）化合物具有药理活性，特别是具有强效驱虫剂作用，或可用作杀虫剂组分的活性成分。因此，本发明涉及含有公式（I）化合物或其盐作为活性成分的药物和杀虫剂组合物。公式（I）化合物中，如果取代基如上所定义，但X代表与亚砜基相对的邻位上的基团--N（R，R1），其中R和R1均代表氢，且R2不是氢、卤素、具有1至6个碳原子的烷基和具有1至6个碳原子的烷氧基，则其酸加成盐为新化合物。这些新化合物也是本发明的对象。
• WOLLWEBER, H.;KOELLING, H.;NIEMERS, E.;WIDDIG, A.;ANDREWS, P.;SCHULZ, H. +, ARZNEIM.-FORSCH., 1984, 34, N 5, 531-542
  作者：WOLLWEBER, H.、KOELLING, H.、NIEMERS, E.、WIDDIG, A.、ANDREWS, P.、SCHULZ, H. +

  DOI：——

  日期：——