10-Oxo-1,5-diaza-bicyclo<4.4.0>dec-5-en | 1784-72-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 10-Oxo-1,5-diaza-bicyclo<4.4.0>dec-5-en
• 英文别名: 2,3,4,7,8,9-hexahydro-pyrido[1,2-a]pyrimidin-6-one；1,5-Diazabicyclo[4.4.0]dec-5-en-10-one；2,3,4,7,8,9-hexahydropyrido[1,2-a]pyrimidin-6-one
• CAS: 1784-72-1
• 化学式: C₈H₁₂N₂O
• 分子量: 152.196
• InChiKey: SENZWMNCHJFUGV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  32.7
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• METHOD FOR PRODUCING 3-SUBSTITUTED-4-FLUOROPYRROLIDINE DERIVATIVE
  申请人：Suzuki Masashi

  公开号：US20130085282A1

  公开（公告）日：2013-04-04

  An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG 1 represents a protecting group for an amino group, R 1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.

  提供了一种廉价且工业上优势的方法，用于生产光学活性的syn-3-(N-取代氨甲基)-4-氟吡咯烷，该化合物可能是生产药物的中间体。本发明涉及一种生产syn-1-保护的-4-氟-3-(N-取代-N-硝基苯磺酰基)吡咯烷衍生物或其对映体或其盐的方法，包括将通式（6）所代表的化合物（其中，PG1代表氨基的保护基，R1代表可取代的C1到C6烷基或可取代的C3到C8环烷基，Ns代表2-硝基苯磺酰基或4-硝基苯磺酰基）或其对映体使用亲核氟化试剂和具有酰胺或鸟嘌呤结构的有机碱进行氟化的过程。
• Curable composition, image forming material, and planographic printing plate precursor
  申请人：FUJIFILM Corporation

  公开号：EP2042522A1

  公开（公告）日：2009-04-01

  A curable composition in which polymerization inhibition due to oxygen is suppressed and which may be cured with high sensitivity by exposure to laser light or the like is provided. The curable composition includes: a polymerizable compound having an ethylenically unsaturated bond; a binder; a radical polymerization initiator; and at least one specific amine compound. Also provided is an image forming material and a negative-working planographic printing plate precursor including the curable composition.

  本发明提供了一种可固化组合物，该组合物抑制了氧气引起的聚合抑制，并可通过激光或类似光源进行高灵敏度固化。这种可固化组合物包括：具有乙烯不饱和键的可聚合化合物；粘合剂；自由基聚合引发剂；以及至少一种特定的胺化合物。此外，还提供了一种图像形成材料和一种包括该可固化组合物的底片-工作平版印刷板前体。
• PROCESS FOR PREPARATION OF 3-SUBSTITUTED-4-FLUOROPYRROLIDINE DERIVATIVES
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：EP2578568A1

  公开（公告）日：2013-04-10

  An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG1 represents a protecting group for an amino group, R1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.

  本发明提供了一种生产具有光学活性的合成-3-(N-取代-氨甲基)-4-氟吡咯烷的廉价且具有工业优势的方法，该方法可作为生产药物的中间体。本发明涉及一种生产受 syn-1 保护的-4-氟-3-(N-取代-N-硝基苯磺酰基)吡咯烷衍生物或其对映体或它们的盐的方法，包括将通式 (6) 所代表的化合物氟化的过程（式中，PG1 代表氨基的保护基团、R1 代表可能被取代的 C1 至 C6 烷基或可能被取代的 C3 至 C8 环烷基，Ns 代表 2-硝基苯磺酰基或 4-硝基苯磺酰基）或其对映体，使用亲核氟化剂和具有脒基或胍基结构的有机碱。
• AMIDO COMPOUNDS AS RORYT MODULATORS AND USES THEREOF
  申请人：New York University

  公开号：EP3002008A1

  公开（公告）日：2016-04-06

  Amido compounds are disclosed that have a formula represented by the following: and wherein n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.

  本发明公开了具有下式表示的氨基化合物： 其中 n1、n2、R1a、R1b、R2、R3、R4、R5 和 R6 如本文所述。这些化合物可制备成药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，包括非限制性的炎症、自身免疫性疾病、癌症和移植物抗宿主疾病。
• Amido compounds as RORγt modulators and uses thereof
  申请人：New York University

  公开号：US10561666B2

  公开（公告）日：2020-02-18

  Amido compounds are disclosed that have a formula represented by the following: and wherein n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.

  本发明公开了具有下式表示的氨基化合物： 其中 n1、n2、R1a、R1b、R2、R3、R4、R5 和 R6 如本文所述。这些化合物可制备成药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，包括非限制性的炎症、自身免疫性疾病、癌症和移植物抗宿主疾病。