1-[(4-Methoxyphenyl)diphenylmethoxy]-3-[4-(phenylmethoxy)-phenoxy]-2-propanol | 111841-68-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 1-[(4-Methoxyphenyl)diphenylmethoxy]-3-[4-(phenylmethoxy)-phenoxy]-2-propanol
• 英文别名: 1-[(4-methoxyphenyl)-diphenylmethoxy]-3-(4-phenylmethoxyphenoxy)propan-2-ol
• CAS: 111841-68-0
• 化学式: C₃₆H₃₄O₅
• 分子量: 546.663
• InChiKey: YZOUFPHWKXQRPS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.2
• 重原子数：
  41
• 可旋转键数：
  13
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  57.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-[(4-Methoxyphenyl)diphenylmethoxy]-3-[4-(phenylmethoxy)-phenoxy]-2-propanol 在 amberlyst-15 、 sodium acetate 、 sodium hydride 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 、 四氯化碳 、 氯仿 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 62.5h， 生成 3-(3-{[3-(4-Benzyloxy-phenoxy)-2-methoxy-propoxy]-hydroxy-phosphoryloxy}-benzyl)-thiazol-3-ium
  参考文献：
  名称：

  Analogs of platelet activating factor. 6. Mono- and bis-aryl phosphate antagonists of platelet activating factor

  摘要：

  A series of aryl phosphoglyceride (3, 19-6 1) and bis-aryl phosphate (67-135) antagonists of platelet activating factor (PAF) were prepared. A group of four bifunctional phosphorus reagents (5a-c and 7) were developed that allowed the preparation of these aryl phosphates in which the position of aromatic substitution can be varied. These compounds were examined for their ability to inhibit PAF-induced platelet aggregation of rabbit platelets. Selected compounds were also evaluated for their ability to displace [H-3]PAF from its receptor on rabbit platelets. These in vitro data were compared to similar data obtained for a number of known PAF antagonists. The compounds were evaluated in vivo, in both the mouse and rabbit, for their ability to prevent death induced by a lethal challenge of PAF. The relationships between the biological activity and the nature, lipophilicity, and position of substituents of the aromatic rings were studied. Compound 105 (CL 184005) has been selected to undergo further development as a potential therapeutic agent for the treatment of septic shock in man.

  DOI：

  10.1021/jm00087a023
• 作为产物：
  描述：

  2,2-dimethyl-4-[[4-(phenylmethoxy)phenoxy]methyl]-1,3-dioxolane 在 吡啶 、 硫酸 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 19.5h， 生成 1-[(4-Methoxyphenyl)diphenylmethoxy]-3-[4-(phenylmethoxy)-phenoxy]-2-propanol
  参考文献：
  名称：

  Analogs of platelet activating factor. 6. Mono- and bis-aryl phosphate antagonists of platelet activating factor

  摘要：

  A series of aryl phosphoglyceride (3, 19-6 1) and bis-aryl phosphate (67-135) antagonists of platelet activating factor (PAF) were prepared. A group of four bifunctional phosphorus reagents (5a-c and 7) were developed that allowed the preparation of these aryl phosphates in which the position of aromatic substitution can be varied. These compounds were examined for their ability to inhibit PAF-induced platelet aggregation of rabbit platelets. Selected compounds were also evaluated for their ability to displace [H-3]PAF from its receptor on rabbit platelets. These in vitro data were compared to similar data obtained for a number of known PAF antagonists. The compounds were evaluated in vivo, in both the mouse and rabbit, for their ability to prevent death induced by a lethal challenge of PAF. The relationships between the biological activity and the nature, lipophilicity, and position of substituents of the aromatic rings were studied. Compound 105 (CL 184005) has been selected to undergo further development as a potential therapeutic agent for the treatment of septic shock in man.

  DOI：

  10.1021/jm00087a023

文献信息

• Antihypertensive phosphate derivatives
  申请人：American Cyanamid Company

  公开号：US04897385A1

  公开（公告）日：1990-01-30

  Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from the group consisting of a phenyl radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen, and a naphthalene radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Y is selected from the group of bivalent radicals consisting of --(CH.sub.2).sub.p -- and --(CHR).sub.p --, wherein p is an integer from 2 to 10 and the moiety --(CHR).sub.p -- represents an alkylene chain substituted with one or more C.sub.1 -C.sub.8 alkyl groups or phenyl groups; Z is selected from the group consisting of ##STR3## wherein q is an integer from 4-7 and R.sub.2 may be the same or different and is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 branched or straight chain alkyl.

  本文描述了具有以下公式的降压磷酸酯衍生物：##STR1## 其中X选自以下组合中的苯基基团，在任意位置用C.sub.1-C.sub.20分支或直链烷氧基或苄氧基取代，且可在任何其他位置用一个或多个由C.sub.1-C.sub.15分支或直链烷基，C.sub.1-C.sub.15分支或直链烷氧基和卤素组成的基团进行取代；或者选自以下组合中的萘基基团，在任意位置用C.sub.1-C.sub.20分支或直链烷氧基或苄氧基取代，且可在任何其他位置用一个或多个由C.sub.1-C.sub.15分支或直链烷基，C.sub.1-C.sub.15分支或直链烷氧基和卤素组成的基团进行取代；T选自以下组合中的氢和##STR2## 其中R.sub.1选自以下组合中的氢，C.sub.1-C.sub.4分支或直链烷基，C.sub.1-C.sub.4分支或直链烷氧基和C.sub.1-C.sub.4分支或直链烷基胺基；Y选自以下双价基团组合中的一种，--（CH.sub.2）.sub.p--和--（CHR）.sub.p--，其中p为2到10的整数，且--（CHR）.sub.p--基团表示带有一个或多个C.sub.1-C.sub.8烷基或苯基的烷基链；Z选自以下组合中的一种##STR3## 其中q为4-7的整数，R.sub.2可以相同也可以不同，并选自以下组合中的氢和C.sub.1-C.sub.4分支或直链烷基。
• US4697031A
  申请人：——

  公开号：US4697031A

  公开（公告）日：1987-09-29
• US4897385A
  申请人：——

  公开号：US4897385A

  公开（公告）日：1990-01-30
• Analogs of platelet activating factor. 6. Mono- and bis-aryl phosphate antagonists of platelet activating factor
  作者：A. Wissner、M. L. Carroll、K. E. Green、S. S. Kerwar、W. C. Pickett、R. E. Schaub、L. W. Torley、S. Wrenn、C. A. Kohler

  DOI：10.1021/jm00087a023

  日期：1992.5

  A series of aryl phosphoglyceride (3, 19-6 1) and bis-aryl phosphate (67-135) antagonists of platelet activating factor (PAF) were prepared. A group of four bifunctional phosphorus reagents (5a-c and 7) were developed that allowed the preparation of these aryl phosphates in which the position of aromatic substitution can be varied. These compounds were examined for their ability to inhibit PAF-induced platelet aggregation of rabbit platelets. Selected compounds were also evaluated for their ability to displace [H-3]PAF from its receptor on rabbit platelets. These in vitro data were compared to similar data obtained for a number of known PAF antagonists. The compounds were evaluated in vivo, in both the mouse and rabbit, for their ability to prevent death induced by a lethal challenge of PAF. The relationships between the biological activity and the nature, lipophilicity, and position of substituents of the aromatic rings were studied. Compound 105 (CL 184005) has been selected to undergo further development as a potential therapeutic agent for the treatment of septic shock in man.