2',6'-diisopropoxy-[1,1'-biphenyl]-2-ylphosphine | 1355317-76-8

• 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',6'-diisopropoxy-[1,1'-biphenyl]-2-ylphosphine
• 英文别名: [2-(2,6-diisopropoxyphenyl)phenyl]phosphane；(2',6'-diisopropoxy-2-biphenylyl)phosphine；(2',6'-diisopropoxybiphenyl-2-yl)phosphine；phosphino-2',6'-di-i-propoxy-1,1'-biphenyl；phosphino-2',6'-diisopropoxy-1,1'-biphenyl；phosphino-2',6'-diisopropoxybiphenyl；[2-[2,6-Di(propan-2-yloxy)phenyl]phenyl]phosphane
• CAS: 1355317-76-8
• 化学式: C₁₈H₂₃O₂P
• 分子量: 302.353
• InChiKey: CMBZOALBSQQXFT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.43
• 重原子数：
  21.0
• 可旋转键数：
  5.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  18.46
• 氢给体数：
  0.0
• 氢受体数：
  2.0

反应信息

• 作为反应物：
  描述：

  2',6'-diisopropoxy-[1,1'-biphenyl]-2-ylphosphine 、 二苄叉丙酮 在 六氟异丙醇 作用下， 以56%的产率得到
  参考文献：
  名称：

  Pd催化的联芳电子膦烷配体与受阻电子缺陷苯胺与大（杂）芳基卤化物的交叉偶联

  摘要：

  由联芳基伯膦加成反式，反式衍生的联芳基膦烷配体-二亚苄基丙酮（AlisonPhos和AliPhos）形成受阻电子缺陷苯胺与受阻（杂）芳基卤化物的钯催化偶联的高活性配体，这是一类具有挑战性的C-N交叉偶联反应，几乎没有先例。在反应条件下观察到较宽的底物范围和官能团耐受性。计算研究表明，与烷基取代的膦亚胺相比，含苯基取代基的配体通过更有利的苯胺键合在催化循环中提供更大的活性。在1,1,1,1,3,3,3-六氟异丙醇（HFIP）中，通过将伯联芳基膦在1,1,1,3,3,3-六氟异丙醇（HFIP）中的磷-迈克尔加成反应，合成联芳基膦酸酯的一般和高产程序还描述了相对温和的条件（23–110°C）。

  DOI：

  10.1021/acscatal.0c04280
• 作为产物：
  描述：

  2-溴氯苯 在 lithium aluminium tetrahydride 、 正丁基锂 作用下， 以 正己烷 为溶剂， 生成 2',6'-diisopropoxy-[1,1'-biphenyl]-2-ylphosphine
  参考文献：
  名称：

  手性单齿膦和大宗羧酸：在钯催化的对映选择性C（sp3）–H功能化中的协同作用

  摘要：

  联手：重要的二氢吲哚骨架在钯（0）催化的芳基三氟甲磺酸酯的C（sp 3）–H活化中的对映体比率高达98：2 。关键是富电子的单齿鼠尾草和庞大的9 H-蒽并9-9羧酸的组合。两者都以高度合作的方式参与对映确定一致的去质子化金属化步骤（参见方案，Tf = triflate）。

  DOI：

  10.1002/anie.201108511

文献信息

• EUROPIUM COMPLEX
  申请人：TOSOH CORPORATION

  公开号：US20200354389A1

  公开（公告）日：2020-11-12

  To provide europium complexes having high photostability. A europium complex expressed with the following formula (A): wherein, R A and R B are independently a cyclic alkyl group with 3 to 10 carbons, respectively, and R C is a cyclic alkyl group with 3 to 10 carbons or a phenyl group expressed with the following formula (B): (wherein, X A , X B , A C , X D and X E independently represent a hydrogen atom; a fluorine atom; an alkyl group with 1 to 3 carbon(s); an alkyloxy group with 1 to 3 carbon(s); an aryloxy group with 6 to 10 carbons; a fluoroalkyl group with 1 to 3 carbon(s); a fluoroalkyloxy group with 1 to 3 carbon(s); or a phenyl group that may be substituted with a fluorine atom, an alkyl group with 1 to 3 carbon(s), an alkyloxy group with 1 to 3 carbon(s), a fluoroalkyl group with 1 to 3 carbon(s), a fluoroalkyloxy group with 1 to 3 carbon(s), a fluorophenyl group, a hydroxyl group or a cyano group, respectively); R A is a cyclic alkyl group with 3 to 10 carbons; R B and R C are a phenyl group expressed with the formula (B), provided, however, that a case where R A a cyclohexyl group, and, R B and R C are a phenyl group is excluded; or R A , R B and R C independently represent an ortho-substituted phenyl group expressed with the following formula (Ba): (wherein, X E represents a hydrogen atom, an alkyl group with 1 to 3 carbon(s), an alkyloxy group with 1 to 3 carbon(s), a fluoroalkyl group with 1 to 3 carbon(s), a fluoroalkyloxy group with 1 to 3 carbon(s), a naphthyl group that may be substituted with a fluorine atom, a pyridyl group that may be substituted with a fluorine atom, or a phenyl group that is expressed with a formula (C): [wherein, Z A , Z C and Z E independently represent a hydrogen atom, a fluorine atom, an alkyl group with 1 to 3 carbon(s), an alkyloxy group with 1 to 3 carbon(s), a fluoroalkyl group with 1 to 3 carbon(s), a fluoroalkyloxy group with 1 to 3 carbon(s), a phenyl group that may be substituted with a fluorine atom, a hydroxyl group or a cyano group; Z B and Z D independently represent a hydrogen atom or a fluorine atom, respectively], provided, however, that a case where R A , R B and R C are all a phenyl group is excluded), respectively; R D represents a hydrogen atom, a deuterium atom or a fluorine atom; W A and W B independently represent an alkyl group with 1 to 6 carbon(s), a fluoroalkyl group with 1 to 6 carbon(s), a phenyl group, a 2-thienyl group or a 3-thienyl group; and ‘n’ represents an integer of 1 to 3}.

  提供具有高光稳定性的铕配合物。 以下是用以下公式（A）表示的铕配合物： 其中，R A 和R B 分别独立地是具有3至10个碳原子的环烷基基团，而R C 是具有3至10个碳原子的环烷基基团或用以下公式（B）表示的苯基团： （其中，X A 、X B 、A C 、X D 和X E 独立地代表氢原子；氟原子；具有1至3个碳原子的烷基基团；具有1至3个碳原子的烷氧基团；具有6至10个碳原子的芳基氧基团；具有1至3个碳原子的氟烷基基团；具有1至3个碳原子的氟烷氧基团；或者可能被氟原子、具有1至3个碳原子的烷基基团、具有1至3个碳原子的烷氧基团、具有1至3个碳原子的氟烷基基团、具有1至3个碳原子的氟烷氧基团、氟苯基团、羟基或氰基取代的苯基团，分别）； R A 是具有3至10个碳原子的环烷基基团； R B 和R C 是用公式（B）表示的苯基团，但是，排除R A 为环己基团，且R B 和R C 为苯基团的情况；或者 R A ，R B 和R C 独立地表示用以下公式（Ba）表示的邻位取代的苯基团： （其中，X E 代表氢原子、具有1至3个碳原子的烷基基团、具有1至3个碳原子的烷氧基团、具有1至3个碳原子的氟烷基基团、具有1至3个碳原子的氟烷氧基团、可能被氟原子取代的萘基团、可能被氟原子取代的吡啶基团，或者用以下公式（C）表示的苯基团： [其中，Z A 、Z C 和Z E 独立地代表氢原子、氟原子、具有1至3个碳原子的烷基基团、具有1至3个碳原子的烷氧基团、具有1至3个碳原子的氟烷基基团、具有1至3个碳原子的氟烷氧基团、可能被氟原子取代的苯基团、羟基或氰基；Z B 和Z D 独立地代表氢原子或氟原子，但排除R A ，R B 和R C 都是苯基团的情况），分别；R D 代表氢原子、氘原子或氟原子；W A 和W B 独立地表示具有1至6个碳原子的烷基基团、具有1至6个碳原子的氟烷基基团、苯基、2-噻吩基团或3-噻吩基团；‘n’表示1至3的整数。
• PHOSPHINE LIGANDS FOR CATALYTIC REACTIONS
  申请人：Shekhar Shashank

  公开号：US20120022252A1

  公开（公告）日：2012-01-26

  The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands.

  本公开涉及：(a)磷环配体；(b)使用此类磷环配体进行键合反应的方法；以及(c)制备磷环配体的方法。
• Pyridine derivatives
  申请人：Astellas Pharma Inc.

  公开号：US10005762B2

  公开（公告）日：2018-06-26

  The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

  本发明要解决的问题是提供一种适用于药物组合物的化合物，特别是一种治疗夜尿症的药物。 本发明者假定，抑制胎盘亮氨酸氨肽酶（P-LAP）（即裂解 AVP 的氨肽酶）的夜间活性将维持和/或增加内源性 AVP 水平，从而增强抗利尿作用，这将有助于减少夜间排尿次数，并对抑制 P-LAP 的化合物进行了广泛研究。结果，本发明人发现(2R)-3-氨基-2-(吡啶基甲基)-2-羟基丙酸衍生物具有极佳的 P-LAP 抑制活性。本发明者评估了水负荷大鼠的抗利尿作用，发现这些化合物通过抑制 P-LAP 增加了内源性 AVP 水平，从而减少了尿量。因此，本发明提供的化合物有望用作基于 P-LAP 抑制作用的夜尿症治疗剂。
• Substituted fused pyrazole compounds and their use as LRRK2 inhibitors
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：US10975081B2

  公开（公告）日：2021-04-13

  Disclosed are substituted fused pyrazoles, for example substituted indazoles, that inhibit LRRK2 kinase activity, pharmaceutical compositions containing them and their use in the treatment of Parkinson's disease.

  本发明公开了可抑制 LRRK2 激酶活性的取代融合吡唑（例如取代吲唑）、含有它们的药物组合物以及它们在帕金森病治疗中的用途。
• Europium complex
  申请人：TOSOH CORPORATION

  公开号：US10988494B2

  公开（公告）日：2021-04-27

  To provide europium complexes having high photostability. A europium complex expressed with the following formula (A): wherein, RA and RB are independently a cyclic alkyl group with 3 to 10 carbons, respectively, and RC is a cyclic alkyl group with 3 to 10 carbons or a phenyl group expressed with the following formula (B): (wherein, XA, XB, AC, XD and XE independently represent a hydrogen atom; a fluorine atom; an alkyl group with 1 to 3 carbon(s); an alkyloxy group with 1 to 3 carbon(s); an aryloxy group with 6 to 10 carbons; a fluoroalkyl group with 1 to 3 carbon(s); a fluoroalkyloxy group with 1 to 3 carbon(s); or a phenyl group that may be substituted with a fluorine atom, an alkyl group with 1 to 3 carbon(s), an alkyloxy group with 1 to 3 carbon(s), a fluoroalkyl group with 1 to 3 carbon(s), a fluoroalkyloxy group with 1 to 3 carbon(s), a fluorophenyl group, a hydroxyl group or a cyano group, respectively); RA is a cyclic alkyl group with 3 to 10 carbons; RB and RC are a phenyl group expressed with the formula (B), provided, however, that a case where RA a cyclohexyl group, and, RB and RC are a phenyl group is excluded; or RA, RB and RC independently represent an ortho-substituted phenyl group expressed with the following formula (Ba): (wherein, XE represents a hydrogen atom, an alkyl group with 1 to 3 carbon(s), an alkyloxy group with 1 to 3 carbon(s), a fluoroalkyl group with 1 to 3 carbon(s), a fluoroalkyloxy group with 1 to 3 carbon(s), a naphthyl group that may be substituted with a fluorine atom, a pyridyl group that may be substituted with a fluorine atom, or a phenyl group that is expressed with a formula (C): [wherein, ZA, ZC and ZE independently represent a hydrogen atom, a fluorine atom, an alkyl group with 1 to 3 carbon(s), an alkyloxy group with 1 to 3 carbon(s), a fluoroalkyl group with 1 to 3 carbon(s), a fluoroalkyloxy group with 1 to 3 carbon(s), a phenyl group that may be substituted with a fluorine atom, a hydroxyl group or a cyano group; ZB and ZD independently represent a hydrogen atom or a fluorine atom, respectively], provided, however, that a case where RA, RB and RC are all a phenyl group is excluded), respectively; RD represents a hydrogen atom, a deuterium atom or a fluorine atom; WA and WB independently represent an alkyl group with 1 to 6 carbon(s), a fluoroalkyl group with 1 to 6 carbon(s), a phenyl group, a 2-thienyl group or a 3-thienyl group; and ‘n’ represents an integer of 1 to 3}.

  提供具有高光稳定性的铕络合物。 用下式（A）表示的铕络合物： 其中，RA 和 RB 分别独立地为含 3 至 10 个碳原子的环状烷基，RC 为含 3 至 10 个碳原子的环状烷基或苯基，如下式（B）所示： (其中，XA、XB、AC、XD 和 XE 分别代表氢原子；氟原子；含 1 至 3 个碳原子的烷基；含 1 至 3 个碳原子的烷氧基；含 6 至 10 个碳原子的芳氧基；含 1 至 3 个碳原子的氟烷基；含 1 至 3 个碳原子的氟烷氧基；或可分别被氟原子、1 至 3 个碳原子的烷基、1 至 3 个碳原子的烷氧基、1 至 3 个碳原子的氟烷基、1 至 3 个碳原子的氟烷氧基、氟苯基、羟基或氰基取代的苯基）； RA 是含 3 至 10 个碳原子的环状烷基； RB 和 RC 是用式（B）表示的苯基，但不包括 RA 是环己基，RB 和 RC 是苯基的情况；或 RA、RB 和 RC 分别代表用下式（Ba）表示的正代苯基： (其中，XE 代表氢原子、含 1 至 3 个碳原子的烷基、含 1 至 3 个碳原子的烷氧基、含 1 至 3 个碳原子的氟烷基、含 1 至 3 个碳原子的氟烷氧基、可被氟原子取代的萘基、可被氟原子取代的吡啶基或以式 (C) 表示的苯基： [其中，ZA、ZC 和 ZE 分别独立地代表氢原子、氟原子、含 1 至 3 个碳原子的烷基、含 1 至 3 个碳原子的烷氧基、含 1 至 3 个碳原子的氟烷基、含 1 至 3 个碳原子的氟烷氧基、可被氟原子、羟基或氰基取代的苯基；ZB和ZD分别独立地代表氢原子或氟原子]，但不包括RA、RB和RC均为苯基的情况；RD分别代表氢原子、氘原子或氟原子；WA和WB分别独立地代表1至6个碳的烷基、1至6个碳的氟烷基、苯基、2-噻吩基或3-噻吩基；以及'n'代表1至3的整数}。