2-hydroxylaminotetrahydropyran | 74287-91-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧烷类
• 英文名称: 2-hydroxylaminotetrahydropyran
• 英文别名: tetrahydropyranyl-hydroxylamine；N-(2-tetrahydropyranyl)hydroxylamine；tetrahydropyran-2-yl-oxyamine；o-tetrahydropyranyl hydroxylamine；tetrahydro-pyran-2-yl-hydroxylamine；2-tetrahydropyranyl hydroxylamine；N-tetrahydropyranyl hydroxylamine；Tetrahydropyranyl hydroxylamine；N-(oxan-2-yl)hydroxylamine
• CAS: 74287-91-5
• 化学式: C₅H₁₁NO₂
• 分子量: 117.148
• InChiKey: UTTMHMHHOULJMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  8
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  41.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-Cbz-1,2,3, 4-tetrahydro-isoquinoline-6-carboxylic acid 、 2-hydroxylaminotetrahydropyran 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 生成 benzyl 6-[(tetrahydro-2H-pyran-2-yloxy)carbamoyl]-3,4-dihydroisoquinoline-2(1H)-carboxylate
  参考文献：
  名称：

  Novel N-substituted tetrahydroisoquinoline/isoindoline hydroxamic acid compounds

  摘要：

  具有特定分子式I的化合物，其中R1、R2、R3、X、Y、r、s、t、u和v的含义如规范中所定义，以及它们的盐、溶剂合物和水合物是新颖有效的HDAC 6抑制剂。

  公开号：

  EP2100879A1

文献信息

• Aralkyl-N-hydroxyureas as inhibitors of 5-lipoxygenase and oxidation of
  申请人：American Home Products Corporation

  公开号：US05468760A1

  公开（公告）日：1995-11-21

  This invention relates to compounds compounds useful in treating diseases mediated by one or more leukotrienes or oxidative modification of low density lipoprotein such as inflammation, bronchoconstriction or atherosclerosis. The compounds of this invention have the formula: ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, fluorine, chlorine, bromine, iodine, C.sub.1 -C.sub.6 alkyl, trifluoromethyl, C.sub.1 -C.sub.6 alkoxy, or C.sub.1 -C.sub.6 trifluoroalkoxy; R.sup.2 and R.sup.4 are hydrogen or methyl independently; R.sup.5 is hydrogen, methyl or hydroxy; X and Z are independently oxygen or sulfur; and Y is --CH.sub.2 --, --CH(CH.sub.3)--, or --CH.dbd.CHCH(CH.sub.3)--.

  这项发明涉及用于治疗由一个或多个白三烯或低密度脂蛋白的氧化修饰介导的疾病，如炎症、支气管痉挛或动脉粥样硬化的化合物。本发明的化合物具有以下结构式：##STR1##其中R.sup.1和R.sup.3分别独立地是氢、氟、氯、溴、碘、C.sub.1 -C.sub.6烷基、三氟甲基、C.sub.1 -C.sub.6烷氧基或C.sub.1 -C.sub.6三氟烷氧基；R.sup.2和R.sup.4分别是氢或甲基；R.sup.5是氢、甲基或羟基；X和Z独立地是氧或硫；Y是--CH.sub.2 --、--CH(CH.sub.3)--或--CH.dbd.CHCH(CH.sub.3)--。
• N-hydroxy-N-[3-[2-(halophenylthio)phenyl]prop-2-enyl]ureas as
  申请人：Eli Lilly and Company

  公开号：US05283361A1

  公开（公告）日：1994-02-01

  This invention relates to N-hydroxy-N-[3-[2-(4'-halophenylthio)phenyl]prop-2-enyl]ureas, formulations containing those compounds and methods of using such compounds as 5-lipoxygenase inhibiting agents.

  本发明涉及N-羟基-N-[3-[2-(4'-卤苯硫基)苯基]丙-2-烯基]脲类化合物，含有这些化合物的配方以及将这些化合物用作5-脂氧合酶抑制剂的方法。
• Reactivity Models of 1-<i>N</i>-Vinyluracil and Synthesis of a New Class of Potential Antiviral Agents by the Use of 1,3-Dipolar Cycloaddition Reactions
  作者：E. Colacino、G. De Luca、A. Liguori、A. Napoli、C. Siciliano、G. Sindona

  DOI：10.1081/ncn-120022624

  日期：2003.10

  By the use of a convergent approach based on 1,3-dipolar cycloaddition reactions between N-protected formylnitrones generated in situ and 1-N-vinyluracil, a new class of 4'-aza-analogues of 2',3'-dideoxynucleosides is synthesized. Competitive reaction for the endocyclic bond of uracil also brings to a new isoxazolidine derivative fused with the pyrimidine nucleus.

  通过使用基于在原位产生的N-保护的甲酰基硝酮和1-N-乙烯基尿嘧啶之间的1,3-偶极环加成反应的收敛方法，得到了新的2'，3'-二脱氧核苷类4'-氮杂类似物。合成的。尿嘧啶内环键的竞争反应也带来了与嘧啶核融合的新异恶唑烷衍生物。
• Benzopyran and benzothiopyran derivatives
  申请人：Recordati S.A., Chemical and Pharmaceutical Company

  公开号：US05403842A1

  公开（公告）日：1995-04-04

  The invention relates to benzopyranone and benzothiopyranone compounds, compositions and methods of use which have adrenergic and serotonergic activity.

  本发明涉及苯并吡喃酮和苯并噻吩酮化合物、组合物和使用方法，其具有肾上腺素能和血清素能活性。
• Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting
  申请人：Abbott Laboratories

  公开号：US04873259A1

  公开（公告）日：1989-10-10

  Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl; wherein X is oxygen, sulfur, SO.sub.2, or NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkoyl, (4) aroyl, or (5) alkylsulfonyl; A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene; n is 1-5; Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) C.sub.1 -C.sub.8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C.sub.1 to C.sub.12 arylalkyl, (15) C.sub.2 to C.sub.12 arylalkenyl, (16) C.sub.1 to C.sub.12 arylalkoxy, (17) C.sub.1 to C.sub.12 arylthioalkoxy, and substituted derivatives of (18) aryl, (19) aryloxy, (20) aroyl, (21) C.sub.1 to C.sub.12 arylalkyl, (22) C.sub.2 to C.sub.12 arylalkenyl, (23) C.sub.1 to C.sub.12 arylalkoxy, or (24) C.sub.1 to C.sub.12 arylthioalkoxy, wherein substituents are selected from halo, nitro, cyano, C.sub.1 to C.sub.12 alkyl, alkoxy, and halosubstituted alkyl; Z is oxygen or sulfur; and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.12 alkoyl, are potent inhibitors of 5- and/or 12-lipoxygenase enzymes. Also disclosed are lipoxygenase inhibiting compositions and a method for inhibiting lipoxygenase activity.

  该公式的化合物：##STR1##其中R.sub.1是（1）氢，（2）C.sub.1到C.sub.4烷基，（3）C.sub.2到C.sub.4烯基或（4）NR.sub.2R.sub.3，其中R.sub.2和R.sub.3分别选择自（1）氢，（2）C.sub.1到C.sub.4烷基和（3）羟基，但R.sub.2和R.sub.3不能同时为羟基；其中X是氧，硫，SO.sub.2或NR.sub.4，其中R.sub.4是（1）氢，（2）C.sub.1到C.sub.6烷基，（3）C.sub.1到C.sub.6烷酰基，（4）芳酰基或（5）烷基磺酰基；A选择自C.sub.1到C.sub.6烷基和C.sub.2到C.sub.6烯基；n为1-5；Y每次独立选择自（1）氢，（2）卤素，（3）羟基，（4）氰基，（5）卤代烷基，（6）C.sub.1到C.sub.12烷基，（7）C.sub.2到C.sub.12烯基，（8）C.sub.1到C.sub.12烷氧基，（9）C.sub.3到C.sub.8环烷基，（10）C.sub.1-C.sub.8硫代烷基，（11）芳基，（12）芳氧基，（13）芳酰基，（14）C.sub.1到C.sub.12芳基烷基，（15）C.sub.2到C.sub.12芳基烯基，（16）C.sub.1到C.sub.12芳基烷氧基，（17）C.sub.1到C.sub.12芳基硫代烷氧基，以及取代衍生物的（18）芳基，（19）芳氧基，（20）芳酰基，（21）C.sub.1到C.sub.12芳基烷基，（22）C.sub.2到C.sub.12芳基烯基，（23）C.sub.1到C.sub.12芳基烷氧基或（24）C.sub.1到C.sub.12芳基硫代烷氧基，其中取代基选择自卤素，硝基，氰基，C.sub.1到C.sub.12烷基，烷氧基和卤代烷基；Z是氧或硫；M是氢，药学上可接受的阳离子，芳酰基或C.sub.1到C.sub.12烷酰基，是5-和/或12-脂氧合酶酶的有效抑制剂。还公开了抑制脂氧合酶活性的脂氧合酶抑制剂组合物和方法。