1-Phenyl-3-(4-phenyl-2-p-tolyl-thiazol-5-yl)-harnstoff | 58314-84-4

• 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: 1-Phenyl-3-(4-phenyl-2-p-tolyl-thiazol-5-yl)-harnstoff
• 英文别名: 1-phenyl-3-(4-phenyl-2-p-tolyl-thiazol-5-yl)-urea；1-Phenyl-3-[4-phenyl-2-(p-tolyl)-thiazol-5-yl]urea；1-[2-(4-methylphenyl)-4-phenyl-1,3-thiazol-5-yl]-3-phenylurea
• CAS: 58314-84-4
• 化学式: C₂₃H₁₉N₃OS
• 分子量: 385.489
• InChiKey: MOFYKTDWQSQJHG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.04
• 拓扑面积：
  82.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-Phenyl-3-(4-phenyl-2-p-tolyl-thiazol-5-yl)-harnstoff 以75%的产率得到
  参考文献：
  名称：

  WINTERS G.; DI MOLA N., TETRAHEDRON LETT. , 1975, NO 44, 3877-3878

  摘要：

  DOI：

文献信息

• Azole-phenyl urea derivatives as ACAT inhibitors and their production
  申请人：NIHON NOHYAKU CO., LTD.

  公开号：EP0761658A1

  公开（公告）日：1997-03-12

  The present invention relates to azole-phenyl urea derivatives represented by the general formula (I): [wherein each of R1, R2 and R3 is H, halogen, C1-8alkyl or the like, and A is a group represented by the formula (i) or (ii): (wherein R4, R5, R6 and X are as defined in the specification.)] and a pharmacologically acceptable salt thereof, which have ACAT-inhibitory activity and are useful as a prophylactic and therapeutic agent for hypercholesterolemia, atherosclerosis and various diseases caused by them; a process for producing said derivative; and an ACAT inhibitor containing said derivative or salt as an active ingredient.

  本发明涉及一种由通式（I）表示的唑-苯基脲衍生物： [其中R1、R2和R3中的每一个是H、卤素、C1-8烷基或类似物，A是由式（i）或（ii）表示的基团： （其中R4、R5、R6和X如规范中定义。）]及其药理学上可接受的盐，具有ACAT抑制活性，并可用作高胆固醇血症、动脉粥样硬化及由其引起的各种疾病的预防和治疗剂；生产该衍生物的方法；以及含有该衍生物或盐作为活性成分的ACAT抑制剂。
• Fused isoquinoline derivatives
  申请人：Gruppo Lepetit S.p.A.

  公开号：US04113731A1

  公开（公告）日：1978-09-12

  Fused isoquinoline derivatives of the general formula ##STR1## wherein: A is a divalent radical selected from the groups ##STR2## wherein R.sub.3 and R.sub.4 each independently represents hydrogen, alkyl,, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl, cycloalkyl-alkyl or, taken together with the adjacent double bond, represent a cycloalkene containing from 5 to 8 carbon atoms or an aromatic nucleus; R.sub.5 represents hydrogen, hydroxyl, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl or cycloalkyl-alkyl; Y is .dbd.O, .dbd.S or .dbd.NH; X is --O--, --S-- or --NR.sub.6 -- wherein R.sub.6 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl or cycloalkyl-alkyl; R.sub.1 and R.sub.2 each independently represents hydrogen, alkyl, phenyl, cycloalkyl, alkoxy, alkenyloxy, methylenedioxy, cycloalkoxy, halo or di-alkylamino or, taken together with the adjacent carbon atoms of the benzene ring, form a cycloalkenyl group containing 5 or 6 carbon atoms or an aromatic nucleus fused on the benzene ring. The compounds are essentially prepared through thermal cyclization of a compound of the formula ##STR3## wherein A, X, Y, R.sub.1 and R.sub.2 have the same meanings given before, with the proviso that R.sub.1 and R.sub.2 cannot simultaneously occupy both the ortho positions, B represents hydrogen, R represents an --OR.sub.7 or --NR.sub.8 R.sub.9 radical wherein R.sub.7 is alkyl, aryl or aralkyl and R.sub.8 and R.sub.9 each independently represents hydrogen, alkyl, aryl, aralkyl, or taken together with the adjacent nitrogen atom represent a heterocyclic saturated radical of 5 or 6 atoms which may contain a further hetero-atom selected from oxygen and nitrogen, or the symbols B and R taken together represent a further bond between the adjacent carbon and nitrogen atoms.

  通式为##STR1##的熔合异喹啉衍生物，其中：A是从以下组中选择的二价基团##STR2##其中R.sub.3和R.sub.4各自独立地表示氢、烷基、烯基、环烷基、芳基、芳基烷基、芳基烯基、环烷基-烷基或与相邻的双键一起表示含有5至8个碳原子的环烷烯或苯核；R.sub.5表示氢、羟基、烷基、烯基、环烷基、芳基、芳基烷基、芳基烯基或环烷基-烷基；Y是.dbd.O、.dbd.S或.dbd.NH；X是--O--、--S--或--NR.sub.6--，其中R.sub.6表示氢、烷基、环烷基、芳基、芳基烷基或环烷基-烷基；R.sub.1和R.sub.2各自独立地表示氢、烷基、苯基、环烷基、烷氧基、烯基氧基、亚甲二氧基、环烷氧基、卤素或二烷基氨基或与苯环相邻的碳原子一起形成含有5或6个碳原子的环烷烯基或熔合在苯环上的芳香核，但前提是R.sub.1和R.sub.2不能同时占据邻位，B表示氢，R表示--OR.sub.7或--NR.sub.8R.sub.9基团，其中R.sub.7是烷基、芳基或芳基烷基，R.sub.8和R.sub.9各自独立地表示氢、烷基、芳基、芳基烷基，或与相邻的氮原子一起表示含有5或6个原子的饱和杂环基团，该基团可以包含进一步从氧和氮中选择的杂原子，或B和R符号一起表示相邻碳原子和氮原子之间的进一步键。这些化合物基本上是通过化合物的热环化制备而成的，该化合物的通式为##STR3##其中A、X、Y、R.sub.1和R.sub.2具有之前给出的相同含义，但前提是R.sub.1和R.sub.2不能同时占据邻位，B表示氢，R表示--OR.sub.7或--NR.sub.8R.sub.9基团，其中R.sub.7是烷基、芳基或芳基烷基，R.sub.8和R.sub.9各自独立地表示氢、烷基、芳基、芳基烷基，或与相邻的氮原子一起表示含有5或6个原子的饱和杂环基团，该基团可以包含进一步从氧和氮中选择的杂原子，或符号B和R一起表示相邻碳原子和氮原子之间的进一步键。
• US4113731A
  申请人：——

  公开号：US4113731A

  公开（公告）日：1978-09-12