2-amino-4-(dimethylamino)-pyridine | 50426-31-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-amino-4-(dimethylamino)-pyridine
• 英文别名: 4-N,4-N-dimethylpyridine-2,4-diamine
• CAS: 50426-31-8
• 化学式: C₇H₁₁N₃
• mdl: MFCD18384431
• 分子量: 137.184
• InChiKey: QEDNABCLVCJRLV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.285
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险性防范说明：
  P261,P264,P270,P271,P280,P301+P312,P302+P352,P304+P340,P305+P351+P338,P330,P332+P313,P337+P313,P362,P403+P233,P405,P501
• 危险性描述：
  H302,H312,H315,H319,H332,H335
• 储存条件：
  室温

反应信息

• 作为反应物：
  描述：

  1,3-二亚胺基异吲哚啉 、 2-amino-4-(dimethylamino)-pyridine 以 正丁醇 为溶剂， 以11 %的产率得到2-N-[3-[4-(dimethylamino)pyridin-2-yl]iminoisoindol-1-yl]-4-N,4-N-dimethylpyridine-2,4-diamine
  参考文献：
  名称：

  NIR-磷光 Cr(III) 配合物的能隙定律

  摘要：

  一系列含有取代的阴离子 1,3-双（吡啶-2-基亚氨基）异吲哚啉-2-ide 配体的均配 Cr(III) 配合物在脱气流体溶液中发出磷光，λmax在777–970 nm 范围内。能隙定律已成功应用于 Cr( III ) 配合物的双重激发态。

  DOI：

  10.1039/d2dt02872g
• 作为产物：
  描述：

  3-溴-4-N,N-二甲氨基吡啶 在 potassium amide 、 锌 作用下， 以 乙醚 、 氨 、 溶剂黄146 为溶剂， 反应 3.5h， 生成 2-amino-4-(dimethylamino)-pyridine
  参考文献：
  名称：

  Groziak, Michael P.; Melcher, Laura M., Heterocycles, 1987, vol. 26, # 11, p. 2905 - 2910

  摘要：

  DOI：

文献信息

• [EN] QUINAZOLINE DERIVATIVES<br/>[FR] DERIVES DE QUINAZOLINE
  申请人：ASTRAZENECA AB

  公开号：WO2006040520A1

  公开（公告）日：2006-04-20

  The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.

  这项发明涉及式(I)的喹唑啉衍生物或其药用盐、溶剂化合物或前药，其中X1、p、R1、q、R2、R3、R4、R5、环A、r和R6中的每一个在描述中已定义的含义中具有任何含义；它们的制备方法，含有它们的药物组合物以及它们在制造用于治疗细胞增殖紊乱或与血管生成和/或血管通透性相关的疾病状态的药物的用途。
• [EN] SUBSTITUTED TRIAZOLES AND THEIR USE FOR TREATMENT AND/OR PREVENTION NEUROLOGICAL AND PSYCHIATRIC DISORDERS<br/>[FR] TRIAZOLES SUBSTITUÉS ET LEUR UTILISATION POUR LE TRAITEMENT ET/OU LA PRÉVENTION DE TROUBLES NEUROLOGIQUES ET PSYCHIATRIQUES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2013107761A1

  公开（公告）日：2013-07-25

  This invention relates to compounds of formula (I), their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.

  这项发明涉及式(I)的化合物，它们作为mGlu5受体活性的正向变构调节剂的用途，含有这些化合物的药物组合物，以及将其用作治疗和/或预防与谷氨酸功能障碍相关的神经和精神疾病，如精神分裂症或认知功能下降，如痴呆症或认知障碍的药剂的方法。A、B、Ar、R1、R2、R3在描述中有给定的含义。
• [EN] INHIBITORS OF BRUTON'S TYROSINE KINASE<br/>[FR] INHIBITEURS DE LA TYROSINE KINASE DE BRUTON
  申请人：PHARMACYCLICS LLC

  公开号：WO2016004272A1

  公开（公告）日：2016-01-07

  Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

  本文披露了抑制布鲁顿酪氨酸激酶（Btk）的化合物。还描述了Btk的不可逆抑制剂。此外，还描述了Btk的可逆抑制剂。还披露了包括这些化合物的药物组合物。披露了使用Btk抑制剂的方法，单独或与其他治疗剂联合治疗自身免疫疾病或症状、异源免疫疾病或症状、癌症（包括淋巴瘤）和炎症性疾病或症状。
• Chiral Pyridinium Phosphoramide as a Dual Brønsted Acid Catalyst for Enantioselective Diels–Alder Reaction
  作者：Yasuhiro Nishikawa、Saki Nakano、Yuu Tahira、Kanako Terazawa、Ken Yamazaki、Chitoshi Kitamura、Osamu Hara

  DOI：10.1021/acs.orglett.6b00608

  日期：2016.5.6

  Chiral pyridinium phosphoramide 1·HX was designed to be a new class of chiral Brønsted acid catalyst in which both the pyridinium proton and the adjacent imide-like proton activated by the electron-withdrawing pyridinium moiety could work cooperatively as strong dual proton donors. The potential of 1·HX was shown in the enantioselective Diels–Alder reactions of 1-amino dienes with various dienophiles

  手性吡啶鎓磷酰胺1·HX被设计为一类新型的手性布朗斯台德酸催化剂，其中吡啶电子质子和由吸电子吡啶鎓部分活化的相邻的酰亚胺样质子都可以作为强的双质子供体协同工作。1-氨基二烯与包括N-未取代的马来酰亚胺在内的各种亲二烯体的对映选择性Diels-Alder反应显示了1·HX的潜力，该反应尚未成功地用于不对称Diels-Alder反应。
• [EN] 2-PHENYL OR 2-HETARYL IMIDAZOL[1,2-a]PYRIDINE DERIVATIVES<br/>[FR] DÉRIVÉS DE 2-PHÉNYL- OU 2-HÉTARYL-IMIDAZOL[1,2-A]PYRIDINE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2014177458A1

  公开（公告）日：2014-11-06

  The invention relates to compounds of formulas I and II, formula I or formula II wherein R1 is hydrogen, lower alkyl, lower alkoxy, halogen, S-lower alkyl, lower alkoxy substituted by halogen, di-lower alkyl amino, C(O)O-lower alkyl, lower alkyl substituted by hydroxy or hydroxy; R2 is hydrogen, lower alkyl, halogen, lower alkoxy, S-lower alkyl, lower alkoxy substituted by halogen, O(CH2)2-lower alkoxy substituted by halogen, di-lower alkyl amino, alkyl amino, NH-lower alkyl substituted by halogen, N(lower alkyl)-benzyl, lower alkyl substituted by hydroxy, heterocycloalkyl optionally substituted by halogen, CH2-lower alkoxy, CH2-lower alkoxy substituted by halogen or hydroxy; or R1 and R2 form together with the carbon atoms to which they are attached a ring containing -OCH2CH2O-, OCH2O-, OCH2CH2CH2O- or -NHC(O)CH2O-; R3 is hydrogen or lower alkoxy; R4 is hydrogen or lower alkyl; R5 is lower alkyl, cycloalkyl, lower alkyl substituted by hydroxy or lower alkyl substituted by halogen; or R4 and R5 form together with the nitrogen atom to which they are attached a ring containing -CH2CH2CHRCH2CH2-, -CH2CHRCH2CH2-, -CH2CH2OCH2CH2-, -CH2CH2NR'CH2CH2-, CH2CHR- or -CH2CH2CH2-; wherein R is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R' is lower alkyl substituted by halogen; Ra is hydrogen or H; Rb is hydrogen, hydroxy or 3H; R6 is hydrogen, halogen or lower alkyl; HetAr is selected from the group consisting of thiophenyl, furanyl, thiozolyl, benzofuranyl, pyrazolyl, benzoimidazolyl or pyridinyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The present compounds are suitable as imaging tool, which will improve diagnosis by identifying potential patients with excess of tau aggregates in the brain, which may be likely to develop Alzheimer's disease.

  本发明涉及式I和式II的化合物，式I或式II中，R1为氢、低级烷基、低级烷氧基、卤素、S-低级烷基、卤素取代的低级烷氧基、二-低级烷基氨基、C(O)O-低级烷基、羟基取代的低级烷基或羟基；R2为氢、低级烷基、卤素、低级烷氧基、S-低级烷基、卤素取代的低级烷氧基、O(CH2)2-卤素取代的低级烷氧基、二-低级烷基氨基、烷基氨基、NH-卤素取代的低级烷基、N(低级烷基)-苄基、羟基取代的低级烷基、任选卤素取代的杂环烷基、CH2-低级烷氧基、CH2-卤素或羟基取代的低级烷氧基；或者R1和R2与其所连接的碳原子一起形成含有-OCH2CH2O-、OCH2O-、OCH2CH2CH2O-或-NHC(O)CH2O-的环；R3为氢或低级烷氧基；R4为氢或低级烷基；R5为低级烷基、环烷基、羟基取代的低级烷基或卤素取代的低级烷基；或者R4和R5与其所连接的氮原子一起形成含有-CH2CH2CHRCH2CH2-、-CH2CHRCH2CH2-、-CH2CH2OCH2CH2-、-CH2CH2NR'CH2CH2-、CH2CHR-或-CH2CH2CH2-的环；其中R为氢、卤素、低级烷基、低级烷氧基或卤素取代的低级烷基；R'为卤素取代的低级烷基；Ra为氢或H；Rb为氢、羟基或3H；R6为氢、卤素或低级烷基；HetAr选自噻吩基、呋喃基、噻唑基、苯并呋喃基、吡唑基、苯并咪唑基或吡啶基；n为1或2；或为药学上可接受的酸加成盐、外消旋混合物或其相应的对映体和/或光学异构体。本发明的化合物适合作为成像工具，通过识别大脑中tau聚集体过量的潜在患者，将有助于改善诊断，这些患者可能发展为阿尔茨海默病。