6,7-Dichloro-3,4-dihydro-4-methyl-2H-pyrazino(2,3-b)(1,4)oxazine | 63880-12-6

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 6,7-Dichloro-3,4-dihydro-4-methyl-2H-pyrazino(2,3-b)(1,4)oxazine
• 英文别名: 6,7-dichloro-4-methyl-2,3-dihydropyrazino[2,3-b][1,4]oxazine
• CAS: 63880-12-6
• 化学式: C₇H₇Cl₂N₃O
• 分子量: 220.058
• InChiKey: FNTCIOUNVBAMSM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  38.2
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  monomethyl-amino-ethanol 、 四氯吡嗪 、 2-[methyl-(3,5,6-trichloro-pyrazin-2-yl)-amino]-ethanol 在 sodium 作用下， 以 乙醇 为溶剂， 以27%的产率得到6,7-Dichloro-3,4-dihydro-4-methyl-2H-pyrazino(2,3-b)(1,4)oxazine
  参考文献：
  名称：

  6,7-Dichloro-3,4-dihydro-2H-pyrazino(2,3-B)(1,4)oxazines

  摘要：

  公开了式子为##STR1##其中R为H或C.sub.1到C.sub.8烷基，烯基，环烷基或环烯基基团的二氯吡嗪-氧杂环化合物。R为H的化合物具有作为R不为H的化合物的中间体的实用性。后者化合物表现出微生物杀灭，除草或杀虫活性。本发明的化合物可以从四氯吡嗪和R-NH-CH.sub.2 CH.sub.2 -OH的2-氨基乙醇中轻松制备。

  公开号：

  US04029657A1

文献信息

• Chemokine Receptor Antagonist and Medical Use Thereof
  申请人：Habashita Hiromu

  公开号：US20070254886A1

  公开（公告）日：2007-11-01

  The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.), and the like], and the like.

  本发明涉及一种由公式（I）表示的化合物，其盐、N-氧化物、溶剂化物或前药，以及其医药用途（公式中的符号如说明书所述）。公式（I）表示的化合物具有趋化因子受体（尤其是在CCR4和/或CCR5中）拮抗活性。因此，它对于预防和/或治疗趋化因子受体介导的疾病，如炎症和/或过敏性疾病[全身性炎症反应综合征（SIRS）、过敏性休克、过敏性反应、过敏性血管炎、移植排斥反应、肝炎、肾炎、肾病、胰腺炎、鼻炎、关节炎、炎症性眼部疾病、炎症性肠病、脑和/或循环系统疾病、呼吸系统疾病、皮肤病、自身免疫性疾病等]、感染[病毒性疾病（人类免疫缺陷病毒感染、获得性免疫缺陷综合征、SARS等）等]等非常有用。
• CHEMOKINE RECEPTOR ANTAGONIST AND MEDICAL USE THEREOF
  申请人：HABASHITA Hiromu

  公开号：US20100266539A1

  公开（公告）日：2010-10-21

  The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.), and the like], and the like.

  本发明涉及一种由式（I）所表示的化合物，其盐、N-氧化物、溶剂化物或前药，以及其医药用途（式中符号如规范所述）。由式（I）所表示的化合物具有趋化因子受体（特别是在CCR4和/或CCR5中）的拮抗活性。因此，它对于预防和/或治疗趋化因子受体介导的疾病，如炎症和/或过敏性疾病[全身性炎症反应综合征（SIRS）、过敏反应、过敏性血管炎、移植排斥反应、肝炎、肾炎、肾病、胰腺炎、鼻炎、关节炎、炎症性眼病、炎症性肠病、脑和/或循环系统疾病、呼吸道疾病、皮肤病、自身免疫性疾病等]、感染[病毒性疾病（人类免疫缺陷病毒感染、获得性免疫缺陷综合征、SARS等）等]等具有用处。
• US4029657A
  申请人：——

  公开号：US4029657A

  公开（公告）日：1977-06-14
• US7732442B2
  申请人：——

  公开号：US7732442B2

  公开（公告）日：2010-06-08
• 6,7-Dichloro-3,4-dihydro-2H-pyrazino(2,3-B)(1,4)oxazines
  申请人：The Dow Chemical Company

  公开号：US04029657A1

  公开（公告）日：1977-06-14

  Dichloropyrazino-oxazines of the formula ##STR1## wherein R is H or a C.sub.1 to C.sub.8 alkyl, alkenyl, cycloalkyl or cycloalkenyl radical, are disclosed. The compound in which R is H has utility as an intermediate for the compounds in which R is other than H. The latter compounds exhibit microbicidal, herbicidal or insecticidal activity. The compounds of the invention are readily prepared from tetrachloropyrazine and 2-aminoethanols of the formula R--NH--CH.sub.2 CH.sub.2 --OH.

  本发明揭示了式为## STR1##的二氯吡嗪-噁唑类化合物，其中R为H或C.sub.1到C.sub.8烷基，烯基，环烷基或环烯基基团。当R为H时，该化合物可用作R不为H的化合物的中间体。后者的化合物表现出微生物杀菌，除草或杀虫活性。本发明的化合物可以从四氯吡嗪和R-NH-CH.sub.2 CH.sub.2-OH的2-氨基乙醇式轻松制备。