1-N-Boc-2-indanol | 218151-64-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: 1-N-Boc-2-indanol
• 英文别名: Tert-butyl N-(2-hydroxy-2,3-dihydro-1H-inden-1-YL)carbamate
• CAS: 218151-64-5
• 化学式: C₁₄H₁₉NO₃
• 分子量: 249.31
• InChiKey: ROUONLKDWVQKNB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  58.6
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-N-Boc-2-indanol 在 三乙烯二胺 、 三乙胺 、 对甲苯磺酰氯 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 、 盐酸 、 水 作用下， 以 二氯甲烷 、 甲苯 为溶剂， 以70.3 %的产率得到1-aminoindene
  参考文献：
  名称：

  CN116396189

  摘要：

  公开号：
• 作为产物：
  描述：

  二碳酸二叔丁酯 、 1-氨基-2-茚醇 在 sodium hydroxide 作用下， 以 二氯甲烷 、 水 为溶剂， 生成 1-N-Boc-2-indanol
  参考文献：
  名称：

  CN116396189

  摘要：

  公开号：

文献信息

• [EN] INDOLAMIDE DERIVATIVES WHICH POSSESS GLYCOGEN PHOSPHORYLASE INHIBITORY ACTIVITY<br/>[FR] DERIVES D'INDOLAMIDE POSSEDANT UNE ACTIVITE INHIBITRICE DE LA GLYCOGENE PHOSPHORYLASE
  申请人：ASTRAZENECA AB

  公开号：WO2005020985A1

  公开（公告）日：2005-03-10

  A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; wherein: A is phenylene or heteroarylene; n is 0, 1 or 2; m is 0, 1 or 2; R' is for example selected from halo, nitro, cyano, hydroxy, carboxy, carbamoyl, N-(1-4C)alkylcarbamoyl, N-(1-4C)alkylsulphamoyl, (1-4C)alkyl, (1-4C)alkoxy, (1­4C)alkanoyl, (1-4C)alkanoyloxy, hydroxy(1-4C)alkyl, fluoromethyl, and -NHSO2(1­4C)alkyl; or, when n is 2, the two R1 groups, together with the carbon atoms of A to which they are attached, may form a 4 to 7 membered saturated ring, optionally containing 1 or 2 heteroatoms independently selected from 0, S and N; R2 and R3 together with the nitrogen to which they are attached form an optionally substituted 4- to 7-membered, heterocyclic ring; and R4 is for example halo or (1-4C)alkyl; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.

  该化合物的结构式（1）或其药用盐或前药；其中：A为苯基或杂环烷基；n为0、1或2；m为0、1或2；R'例如选自卤素、硝基、氰基、羟基、羧基、氨基甲酰基、N-（1-4C）烷基甲酰基、N-（1-4C）烷基磺酰基、（1-4C）烷基、（1-4C）烷氧基、（1-4C）烷酰基、（1-4C）烷酰氧基、羟基（1-4C）烷基、氟甲基和-NHSO2（1-4C）烷基；或者，当n为2时，两个R1基团与它们连接的A的碳原子一起可以形成一个含有1或2个杂原子（独立选择自0、S和N）的4到7元饱和环；R2和R3与它们连接的氮形成一个可选择取代的4到7元杂环；R4例如为卤素或（1-4C）烷基；具有糖原磷酸化酶抑制活性，并因此在治疗与糖原磷酸化酶活性增加相关的疾病状态中具有价值。描述了制备该化合物和含有它们的药物组合物的方法。
• Lactam-containing cyclic diamines and derivatives as factor Xa inhibitors
  申请人：——

  公开号：US20040204454A1

  公开（公告）日：2004-10-14

  The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P 4 -M-M 4 I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

  本申请描述了公式I：P4-M-M4I或其药学上可接受的盐形式的含有内酰胺的环状二胺及其衍生物，其中M是非芳香性碳环或杂环。本发明化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa的抑制剂。
• Heterocyclic amide derivatives having glycogen phosphorylase inhibitory activity
  申请人：Whittamore Robert Owen Paul

  公开号：US20050131052A1

  公开（公告）日：2005-06-16

  Heterocyclic amides of formula (1) wherein: Z is CH or nitrogen; R 4 and R 5 together are either —S—C(R 6 )═C(R 7 )— or —C(R 7 )═C(R 6 )—S—; R 6 and R 7 are selected from for example hydrogen, halo, C 1-4 alkyl, and C 1-4 alkanoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R 1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; r is 1 or 2; Y is —NR 2 R 3 or —OR 3 ; R 2 and R 3 are selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C 1-4 alkyl(optionally substituted by 1 or 2 R 8 groups); R 4 is selected from for example hydrogen, halo, nitro, cyano, hydroxy, C 1-4 alkyl, and C 1-4 alkanoyl; R 8 is selected from for example hydroxy, —COCOOR 9 , —C(O)N(R 9 )(R 10 ), —NHC(O)R 9 , (R 9 )(R 10 )N— and —COOR 9 ; R 9 and R 10 are selected from for example hydrogen, hydroxy, C 1-4 alkyl (optionally substituted by 1 or 2 R 13 ); R 13 is selected from hydroxy, halo, trihalomethyl and C 1-4 alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

  化合物的异环酰胺式（1），其中：Z为CH或氮；R4和R5一起是—S—C（R6）═C（R7）—或—C（R7）═C（R6）—S—；R6和R7选择自例如氢，卤素，C1-4烷基和C1-4烷酰基；A为苯撑或杂芳撑；n为0，1或2；R1选择自例如卤素，硝基，氰基，羟基，羧基；r为1或2；Y为—NR2R3或—OR3；R2和R3选择自例如氢，羟基，芳基，杂环基和C1-4烷基（可选地被1或2个R8基替代）；R4选择自例如氢，卤素，硝基，氰基，羟基，C1-4烷基和C1-4烷酰基；R8选择自例如羟基，—COCOOR9，—C（O）N（R9）（R10），—NHC（O）R9，（R9）（R10）N—和—COOR9；R9和R10选择自例如氢，羟基，C1-4烷基（可选地被1或2个R13取代）；R13选择自例如羟基，卤素，三卤甲基和C1-4烷氧基；或其药学上可接受的盐或前药；具有糖原磷酸化酶抑制活性，因此在治疗与糖原磷酸化酶活性增加相关的疾病状态方面具有价值。描述了制造该异环酰胺衍生物的工艺和含有它们的制药组合物。
• Heterocyclic amide derivatives which process glycogen phorylase inhibitory activity
  申请人：Bennett Norman Lile Stuart

  公开号：US20060264494A1

  公开（公告）日：2006-11-23

  A compound of the formula (1) or a pharmaceutically-acceptable salt, or pro-drug thereof; (1) wherein, for example: R 4 and R 5 together are either —S—C(R 6 ═C(R 7 )— or —C(R 7 )═C(R 6 )—S—; R 6 and R 7 are independently selected from hydrogen and halo; A is phenylene or heteroarylene; n is 0, 1 or 2; R 1 is halo, cyano or carboxy; R 2 is for example methyl; R 3 is for example selected from halo(1-4C)alkyl, dihalo(1-4C)alkyl, tifluoromethyl, hydroxy(1-4C)alkyl, dihydroxy(2-4C)alkyl, trihydroxy(3-4C)alkyl, cyano(1-4C)alkyl (optionally substituted on alkyl with hydroxy), (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkoxy(1-4C)alkyl, di[(1-4C)alkoxy](1-4C)alkyl, (hydroxy)[(1-4C)alkoxy](1-4C)alkyl; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of compounds and pharmaceutical compositions containing them are described.

  公式（1）的化合物或其药物可接受的盐或前药；（1）其中，例如：R4和R5一起是- S-C（R6═C（R7） -或-C（R7）═C（R6） -S-; R6和R7分别选择氢和卤素; A是苯基或杂环芳基; n为0、1或2; R1为卤素、氰基或羧基; R2为例如甲基; R3例如选择自卤（1-4C）烷基、二卤（1-4C）烷基、三氟甲基、羟基（1-4C）烷基、二羟基（2-4C）烷基、三羟基（3-4C）烷基、氰基（1-4C）烷基（在烷基上可选择性地用羟基取代）、（1-4C）烷氧基（1-4C）烷基、（1-4C）烷氧基（1-4C）烷氧基（1-4C）烷基、二（（1-4C）烷氧基）（1-4C）烷基、（羟基）（（1-4C）烷氧基）（1-4C）烷基; 具有糖原磷酸化酶抑制活性，因此在治疗与糖原磷酸化酶活性增加相关的疾病状态方面具有价值。描述了制备化合物和含有它们的制药组合物的过程。
• LACTAM CONTAINING CYCLIC DIAMINES AND DERIVATIVES AS FACTOR XA INHIBITORS
  申请人：Qiao X Jennifer

  公开号：US20070135428A1

  公开（公告）日：2007-06-14

  The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P 4 -M-M 4 I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

  本申请描述了公式I：P4-M-M4I或其药学上可接受的盐形式的含有内酰胺的环状二胺及其衍生物，其中M为非芳香族碳环或杂环。本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是Xa因子的抑制剂。