3-苯氧基吡咯烷 | 21767-14-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: 3-苯氧基吡咯烷
• 英文名称: 3-phenoxypyrrolidine
• 英文别名: 3-phenoxypyrrolidin
• CAS: 21767-14-6
• 化学式: C₁₀H₁₃NO
• mdl: MFCD08688473
• 分子量: 163.219
• InChiKey: SKHPQIQATRHESG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-苯氧基吡咯烷 在 次氯酸叔丁酯 、 sodium methylate 作用下， 以 甲醇 为溶剂， 生成 α,β-trans-benzamido-β-phenoxyproline tert-butyl amide
  参考文献：
  名称：

  Four-component condensation: a new versatile method for the synthesis of substituted prolyl peptides

  摘要：

  DOI：

  10.1021/ja00385a080
• 作为产物：
  描述：

  tert-butyl 3-phenoxypyrrolidine-1-carboxylate 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 反应 1.0h， 生成 3-苯氧基吡咯烷
  参考文献：
  名称：

  [EN] TREATMENT OF MYC-DRIVEN CANCERS WITH GSPT1 DEGRADERS
  [FR] TRAITEMENT DE CANCERS ENTRAÎNÉS PAR MYC AVEC DES AGENTS DE DÉGRADATION GSPT1

  摘要：

  本公开涉及新的方法来预测癌症患者对GSPT1负调节剂的反应性，从而通过确定患者样本中一个或多个生物标志物的水平来确定GSPT1负调节剂治疗癌症患者的有效性。本公开还涉及这些方法的应用，包括分层癌症恶性程度，特别是识别驱动肿瘤的myc，从而为这些癌症患者设计优化和个性化的治疗方案，以及优化选择患者人群进行相应的临床试验。

  公开号：

  WO2022152822A1

文献信息

• [EN] PYRAZOLO [1, 5 -A] PYRIMIDINES AS ANTIVIRAL AGENTS<br/>[FR] PYRAZOLO[1,5-A]PYRIMIDINES EN TANT QU'AGENTS ANTIVIRAUX
  申请人：GILEAD SCIENCES INC

  公开号：WO2011163518A1

  公开（公告）日：2011-12-29

  The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

  本发明提供了公式I或公式II的化合物：(I)、(II)或其药用可接受的盐或酯，如本文所述。这些化合物及其组合物可用于治疗副粘病毒感染。这些化合物、组合物和方法特别适用于治疗人类呼吸道合胞病毒感染。
• [EN] NOVEL HETEROCYCLIC ACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS<br/>[FR] NOUVEAUX ACRYLAMIDES HÉTÉROCYCLIQUES ET LEUR UTILISATION EN TANT QUE PRODUITS PHARMACEUTIQUES
  申请人：FAB PHARMA SAS

  公开号：WO2011061214A1

  公开（公告）日：2011-05-26

  The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

  这项发明涉及新颖的杂环丙烯酰胺化合物（I），涉及该化合物及其中间体的制备，涉及将该化合物用作抗菌药物以及含有该化合物的药物组合物的用途。
• PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS
  申请人：Borriello Manuela

  公开号：US20130261100A1

  公开（公告）日：2013-10-03

  The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is —O—, —O(C1-C3 alkyl)-; —(C1-C3 alkyl)O—; —C(O)—; —C(═N—O(C1-C3 alkyl))-; —NH— or —NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, —NH(C1-C3alkyl)-; —N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is covalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, endometriosis and migraine.

  该发明涉及式(I)的吡啶酰胺衍生物或其药学上可接受的盐，其中R1和R2独立地为氢、直链或支链(C1-C3)烷基，或者它们结合在一起形成环丙基环；R独立地选自卤素和三氟甲基的群，p为1、2或3；A为C或N；E为式(B)或(C)的基团，其中B为C(O)OH、C(O)O(C1-C3)烷基，C选自式(I)的群，m为1、2或3，n为0或1，W为—O—、—O(C1-C3烷基)-、—(C1-C3烷基)O—、—C(O)—、—C(═N—O(C1-C3烷基))-、—NH—或—NH(C1-C3烷基)-；Ar为苯基，可选地取代一个或多个取代基，选自卤素、三氟甲基、三氟甲氧基、甲基、—NH(C1-C3烷基)-、—N(C1-C3烷基)(C1-C3烷基)-，a为含有一个氮原子的5至7元杂环，与Ar共价键合，可选地含有一个或两个来自N、O和S的杂原子；以及含有1至3个来自S、O和N的杂原子的5-或6元杂芳环，该杂芳环被选自(C1-C3)烷基、(C3-C5)环烷氧基、(C1-C3)烷基羰基的一或两个取代基取代。该发明的化合物可用于制造用于治疗需要使用EP4受体拮抗剂的病理病变的药物，例如治疗急性和慢性疼痛、炎症性疼痛、骨关节炎、与炎症相关的疾病如关节炎、类风湿性关节炎、癌症、子宫内膜异位症和偏头痛。
• [EN] PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS DE PYRIDINAMIDE EN TANT QU'ANTAGONISTES DE RÉCEPTEUR EP4
  申请人：ROTTAPHARM SPA

  公开号：WO2012076063A1

  公开（公告）日：2012-06-14

  The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is -O-, -O(C1-C3 alkyl)-; -(C1-C3 alkyl)O-; -C(O)-; -C(=N-O(C1-C3 alkyl))-; -NH- or -NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, -NH(C1-C3alkyl)-; -N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is convalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-membered heteroaromatic ring containing 1 to 3 heteroatoms selected from S, O e N, such heteroaromatic ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl. The compounds of the invention could be used for manufacturing a medicament for the treatment of pathologies which require the use of an antagonist of the EP4 receptor, such as the treatment of acute and chronic pain, inflammatory pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid artrhritis, cancer, endometriosis and migraine.

  该发明涉及式(I)的吡啶酰胺衍生物或其药学上可接受的盐，其中R1和R2独立地为氢、直链或支链(C1-C3)烷基，或者它们结合在一起形成环丙基环；R独立地选自卤素和三氟甲基的群，p为1、2或3；A为C或N；E为式(B)或(C)的基团，其中B为C(O)OH、C(O)O(C1-C3)烷基，C选自式(I)的群，m为1、2或3，n为0或1，W为-O-、-O(C1-C3烷基)-、-(C1-C3烷基)O-、-C(O)-、-C(=N-O(C1-C3烷基))-、-NH-或-NH(C1-C3烷基)-；Ar为苯基，可选择地取代一个或多个取代基，选自卤素、三氟甲基、三氟甲氧基、甲基、-NH(C1-C3烷基)-、-N(C1-C3烷基)(C1-C3烷基)-，a为含有一个氮原子的5至7元杂环环，与Ar共价键合，可选择地含有一个或两个来自N、O和S的杂原子；以及含有1至3个来自S、O和N的杂原子的5-或6元杂芳环，该杂芳环被选自(C1-C3)烷基、(C3-C5)环烷氧基、(C1-C3)烷基羰基的一或两个取代基取代。该发明的化合物可用于制造用于治疗需要使用EP4受体拮抗剂的病理的药物，例如治疗急性和慢性疼痛、炎症性疼痛、骨关节炎、关节炎、类风湿性关节炎、癌症、子宫内膜异位症和偏头痛。
• [EN] DERIVATIVES OF TRIAZINES AND URACILS, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPEUTICS<br/>[FR] DÉRIVÉS DE TRIAZINES ET D'URACILES, LEUR PRÉPARATION ET LEURS APPLICATIONS EN THÉRAPEUTIQUE HUMAINE
  申请人：PF MEDICAMENT

  公开号：WO2010006962A1

  公开（公告）日：2010-01-21

  The present invention relates to derivatives of general formula I wherein : - W represents nitrogen, - R1 represents: • a hydrogen or a linear or branched C1-C5 alkyl radical or, • a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, • a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, • a C6 2-oxocycloalkyl radical - R2 represents a methyl or heptyl, - m, n are equal to 1, - V represents CH2, - X-Y represents -N- (C=O) -, -CH-O-, - Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.

  本发明涉及一般式I的衍生物，其中： - W代表氮， - R1代表： • 氢或直链或支链C1-C5烷基基团，或者 • 被三氟甲基、腈、羟基、C1-C3烷氧基、C3-C6烷氧基烷氧基、吲哚基、噻吩基、氧硫吩基、C1-C3 N-烷基氨基羰基基团取代的C1-C3烷基基团，或者 • 苯基或吡啶基或萘基，或者选择性地被一个或多个卤素原子、硝基、腈、三氟甲基、乙烯、甲硫基、直链或支链C1-C4烷基、直链或支链C1-C3烷氧基基团取代的噻吩基， • C6 2-氧代环烷基基团 - R2代表甲基或庚基， - m，n等于1， - V代表CH2， - X-Y代表-N- (C=O) -，-CH-O-，- Z代表被一个或多个三氟甲基基团、卤素原子或直链C1-C4烷基基团取代的苯基。