3-methoxytetrahydropyran-4-amine | 1173112-80-5

• 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: 3-methoxytetrahydropyran-4-amine
• 英文别名: 3-Methoxyoxan-4-amine
• CAS: 1173112-80-5
• 化学式: C₆H₁₃NO₂
• mdl: MFCD12087954
• 分子量: 131.175
• InChiKey: OHVYRLNUMZHWIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  9
• 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：
  44.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  tert-butyl 7-[(R)-(tert-butoxycarbonylamino)-7-fluoro-3-(phenoxycarbonylamino)-6-isoquinolyl]-8-methyl-2,3-dihydropyrido[2,3-b][1,4]oxazine-1-carboxylate 、 3-methoxytetrahydropyran-4-amine 在 4-二甲氨基吡啶 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 以94.6%的产率得到tert-butyl 7-[8-(tert-butoxycarbonylamino)-7-fluoro-3-[(3-methoxytetrahydropyran-4-yl)carbamoylamino]-6-isoquinolyl]-8-methyl-2,3-dihydropyrido[2,3-b][1,4]oxazine-1-carboxylate
  参考文献：
  名称：

  8-AMINOISOQUINOLINE COMPOUNDS AND USES THEREOF

  摘要：

  公式（I）的3-羰基氨基异喹啉化合物及其变体，以及它们作为HPK1（造血激酶1）抑制剂的用途被描述。这些化合物在治疗HPK1依赖性疾病和增强免疫应答方面是有用的。还描述了抑制HPK1的方法，治疗HPK1依赖性疾病的方法，增强免疫应答的方法，以及制备3-羰基氨基异喹啉化合物的方法。

  公开号：

  US20200108075A1

文献信息

• [EN] PROCESS FOR THE PREPARATION OF CCR-2 ANTAGONIST<br/>[FR] PROCEDE D'ELABORATION D'ANTAGONISTE VIS-A-VIS DU CCR-2
  申请人：MERCK & CO INC

  公开号：WO2005044795A1

  公开（公告）日：2005-05-19

  The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3- [3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl} cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro- 2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro- 4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol- 1-yl)-1-isopropylcyclopent-2- ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1, 6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)- 4-isopropyl-4-[3-(trifluoromethyl)- 7,8-dihydro-1,6-naphthyridin-6(5H)-yl] carbonyl}cyclopent-2-e n-1-yl)- 3-methoxytetrahydro-2H- pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl- 3-[3-(trifluoromethyl)-7, 8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl} cyclopentyl)[(3S,4S)-3- methoxytetrahydro-2H-pyran-4-yl]amine.

  本发明提供了一种高效的合成方法，用于制备((1R,3S)-3-异丙基-3- [3-(三氟甲基)-7,8-二氢-1,6-萘啶-6(5H)-基]羰基}环戊基)[(3S,4S)-3-甲氧基四氢-2H-吡喃-4-基]胺及其琥珀酸盐。本发明还提供了一种高效的合成方法，用于制备中间体(3R)-3-甲氧基四氢-4H-吡喃-4-酮；(1S,4S)-4-(2,5-二甲基-1H-吡咯-1-基)-1-异丙基环戊-2-烯-1-羧酸；以及3-(三氟甲基)-5,6,7,8-四氢-1,6-萘啶；以及用于制备前体(3S,4S)-N-((1S,4S)-4-异丙基-4-[3-(三氟甲基)-7,8-二氢-1,6-萘啶-6(5H)-基]羰基}环戊-2-烯-1-基)-3-甲氧基四氢-2H-吡喃-4-胺。该发明还在于((1R,3S)-3-异丙基-3-[3-(三氟甲基)-7,8-二氢-1,6-萘啶-6(5H)-基]羰基}环戊基)[(3S,4S)-3-甲氧基四氢-2H-吡喃-4-基]胺的琥珀酸盐的优越性能。
• Novel diazepan derivatives
  申请人：Aebi Johannes

  公开号：US20070249589A1

  公开（公告）日：2007-10-25

  The invention is concerned with novel diazepan derivatives of formula (I) wherein A, X, R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.

  这项发明涉及式（I）的新型二氮杂环己烷衍生物，其中A、X、R3、R4、R5、R6、R8、R9、R10、R11、R12、R13、m和n的定义如描述和索赔中所述，以及其生理上可接受的盐。这些化合物是CCR-2受体、CCR-5受体和/或CCR-3受体的拮抗剂，可用作药物。
• [EN] 3-(6-AMINOPYRIDIN-3-YL)BENZAMIDE DERIVATIVES AS RIPK2 INHIBITORS<br/>[FR] DÉRIVÉS DE 3-(6-AMINOPYRIDIN-3-YL)BENZAMIDE UTILISÉS COMME INHIBITEURS DE RIPK2
  申请人：TAKEDA PHARMACEUTICALS CO

  公开号：WO2022066917A1

  公开（公告）日：2022-03-31

  Disclosed are compounds of Formula (1) and pharmaceutically acceptable salts thereof, wherein L1, R1, R2, R3, R4, R6, R7, R8, R9and X5are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with RIPK2.

  本发明涉及式（1）的化合物及其药学上可接受的盐，其中L1、R1、R2、R3、R4、R6、R7、R8、R9和X5在说明书中有定义。本发明还涉及制备式1化合物的材料和方法，含有它们的药物组合物以及它们用于治疗与RIPK2相关的疾病、紊乱和状态的用途。
• PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
  申请人：Deng Yongqi

  公开号：US20120114739A1

  公开（公告）日：2012-05-10

  The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.

  本发明提供了使用吡唑并[1,5-a]嘧啶化合物抑制mTOR的方法以及使用这些化合物进行治疗、预防、抑制或改善与mTOR相关的一种或多种疾病的方法。
• ISOMANNIDE DERIVATIVES AS INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE
  申请人：SANOFI

  公开号：US20150336979A1

  公开（公告）日：2015-11-26

  The present invention relates to compounds of the formula (I), wherein R1, R11, R12 and X have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They are highly potent and selective soluble epoxide hydrolase inhibitors and are suitable, for example, for the therapy and prophylaxis of renal failure, diabetic nephropathy, type 2 diabetes mellitus, inflammation or could show beneficial effects in pain, dyslipidemia and atherosclerosis. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  本发明涉及式(I)的化合物，其中R1，R11，R12和X具有声明中指示的含义。公式I的化合物是有价值的药理活性化合物。它们是高效、选择性可溶性环氧酶抑制剂，适用于肾衰竭、糖尿病性肾病、2型糖尿病、炎症的治疗和预防，或者在疼痛、血脂异常和动脉粥样硬化方面可能显示出有益的效果。本发明还涉及制备式(I)化合物的方法，它们的用途，特别是作为药物中的活性成分，以及包含它们的制药制剂。