2-chloro-3-(4-methoxybenzoyl)-pyridine

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-chloro-3-(4-methoxybenzoyl)-pyridine
• 英文别名: (2-chloropyridin-3-yl)(4-methoxyphenyl)methanone；2-chloro-3-pyridyl 4-methoxyphenyl ketone；2-chloro-3-(4-methoxybenzoyl)pyridine；(2-chloropyridin-3-yl)-(4-methoxyphenyl)methanone
• 化学式: C₁₃H₁₀ClNO₂
• 分子量: 247.681
• InChiKey: GNFLBUIUZINLAC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  39.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-chloro-3-(4-methoxybenzoyl)-pyridine 在 sodium hydride 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 生成 2-(ethylsulfanyl)-3-[1-(4-methoxyphenyl)ethenyl]pyridine
  参考文献：
  名称：

  利用间断的Pummerer反应合成3-芳基噻吩并[2,3-b]-，-[2,3-c]-或-[3,2-c]吡啶

  摘要：

  已经开发了合成三种类型的噻吩并吡啶的有效方法。因此，3-（1-芳基乙烯基）-2-（乙基亚磺酰基）吡啶，4-（1-芳基乙烯基）-3-（乙基亚磺酰基）吡啶和3-（1-芳基乙烯基）-4-（乙基亚磺酰基）吡啶可可以容易地由三步顺序的各个芳基氯吡啶基酮制备，在过量的乙酸酐中于100至130°C的温度下进行间歇Pummerer反应，得​​到3-芳基噻吩并[2,3- b ]吡啶， 3-芳基噻吩并[3，2- c ]吡啶和3-芳基噻吩并[3，2- c ]吡啶。 噻吩并[2,3- b ]吡啶-噻吩并[2,3- c ]吡啶-噻吩并[3,2- c ]吡啶-Pummerer反应中断-乙酸酐

  DOI：

  10.1055/s-0030-1260152
• 作为产物：
  描述：

  2-氯吡啶 、 对甲氧基苯甲酰氯 在 C₄₆H₈₈Cu₂Li₄N₆O₂S₂ 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 反应 2.0h， 以46%的产率得到2-chloro-3-(4-methoxybenzoyl)-pyridine
  参考文献：
  名称：

  扩展硫代铜酸盐化学中的基序：硫氰酸盐络合物中意外的结构多样性†

  摘要：

  已开发出新的硫代（硫氰酸根）铜盐领域。使用廉价，稳定和安全的CuSCN进行制备，这些复合物显示出Lipshutz型二聚体基序，其具有溶剂依赖性的点基身份。在固态状态下可以看到平面，船形和椅子形的整合器。在解决方案中，可以清楚地看到Lipshutz型结构和Gilman结构。自从2007年定向正交杯化技术问世以来，人们已经开始努力研究酰胺配体的结构反应活性和从Lipshutz型铜酸盐（如（TMP）2 Cu（CN）Li 2（THF））提取碱金属盐的方法。1（TMP = 2,2,6,6-四甲基哌啶）。更换CN的-与SCN -目前正在研究作为改善铜酸锂安全性的一种方法。参考铜酸盐（TMP）2 Cu（CN）Li 2（THP）8（THP =四氢吡喃）的合成和固态结构表征先于硫氰酸盐系列（TMP）2 Cu（SCN）Li 2（L）（L ＝ OEt 2 9，THF 10，THP 11）。对于9-11中的每一个，在亚化学计量的Lewis碱（0

  DOI：

  10.1039/c5dt03882k

文献信息

• 2-halo-pyridines
  申请人：Lacer, S.A.

  公开号：US04614833A1

  公开（公告）日：1986-09-30

  2-Halo-pyridines of the general formula I ##STR1## wherein X is Cl or Br; A is .dbd.0 or ##STR2## Ar is phenyl or substituted phenyl of the general formula ##STR3## in which n is 0, 1, 2 or 3; R is alkyl C.sub.1-4, alkoxy C.sub.1-4, phenoxy, alkylthio C.sub.1-4, halogen especially F and Cl, OH or C.sub.6 H.sub.5 ; and their salts, addition compounds and precursors (prodrugs). Furthermore the invention is directed to the production of these compounds and pharmaceuticals containing them.

  2-卤代吡啶的一般化学式为I，其中X为Cl或Br；A为.dbd.0或Ar；Ar为苯基或一般化学式为##STR3##的取代苯基，其中n为0、1、2或3；R为烷基C.sub.1-4、烷氧基C.sub.1-4、苯氧基、烷硫基C.sub.1-4、卤素特别是F和Cl、羟基或C.sub.6 H.sub.5；以及它们的盐、加合物和前体药物（前药）。此外，本发明涉及这些化合物的制备以及含有它们的药物。
• Pyridine compounds and pharmaceutical use thereof
  申请人：Yoshitomi Pharmaceutical Industries, Ltd.

  公开号：US05001137A1

  公开（公告）日：1991-03-19

  A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.

  揭示了一种具有以下结构式的新型吡啶化合物##STR1##，其中每个符号如说明书中定义的那样，或其盐，具有抑制脯氨酸内肽酶活性的特性，并且适用于药用。
• FUSED PYRAZOLE COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND THEIR MEDICINAL USE
  申请人：Yoshitomi Pharmaceutical Industries, Ltd.

  公开号：EP0338087A1

  公开（公告）日：1989-10-25

  Novel fused pyrazole compounds represented by general formula (I) (wherein X represents =N- or =CH-, R repre­sents H, alkyl, alkoxy or halogen, Y¹ represents α, phenyl or phenyl substituted by halogen, alkyl or alkoxy, Y² represents β, -A²-B², H, alkyl, substituted alkyl, phenyl or phenyl substituted by a substituent selected from the group consisting of halogen, alkyl and alkoxy, provided that at least one of Y¹ and Y² represents α or β, Z¹ and Z² each represents -O-, -S- or -NR³ (wherein R³ represents H or alkyl), A¹ and A² each represents alkylene, B¹ and B² each represents carboxyl, alkoxy­carbonyl or phenylalkoxycarbonyl wherein the phenyl group may optionally be substituted by a substituent selected from the group consisting of halogen, alkyl and alkoxy, acyl, -OH, acyloxy, γ or λ (wherein R¹ and R² represents H, alkyl, dial­kylaminoalkyl, hydroxyalkyl or, when taken together, R¹ and R² represent a group forming a heterocyclic ring together with the adjacent nitrogen atom), and L¹ and L² each represents halogen, alkyl or alkoxy) and salts thereof, a process for their preparation and a medicinal composition containing same are disclosed. The compounds have the action of increa­sing phagocytosis of leucocytes, that of increasing phagocytosis of macrophage, that of restoring the number of leucocytes, that of activating infection protective function, that of improving immunological competence, an antitumor action, etc. ABSTRACT Novel fused pyrazole compounds of the general formula wherein all the symbols are as defined in the specification or its pharmaceutically acceptable salt which possesses a stimulating action on phagocytosis of leukocytes, a stimulating action on phagocytosis of macrophages, a restorative action on leukopenia, a stimulating action on non-specific resistance to infection, an antitumour action, an activating action on immune responses and the like, and therefore is of use as a pharmaceutical.

  通式(I)代表的新型融合吡唑化合物（其中X代表＝N-或＝CH-，R代表H、烷基、烷氧基或卤素，Y¹代表α、苯基或被卤素、烷基或烷氧基取代的苯基，Y²代表β、-A²-B²、H、烷基、取代的烷基、苯基或被选自卤素、烷基和烷氧基的取代基取代的苯基，条件是 Y¹ 和 Y² 中至少有一个代表 α 或 β，Z¹ 和 Z² 各自代表 -O-、-S- 或 -NR³（其中 R³ 代表 H 或烷基），A¹ 和 A² 各自代表亚烷基，B¹ 和 B² 各自代表羧基、烷氧基羰基或苯基烷氧基羰基，其中苯基可任选被选自卤素、烷基和烷氧基、酰基、-OH、酰氧基、γ 或 λ （其中 R¹ 和 R² 代表 H、烷基、二烷基氨基烷基、羟基烷基或）的取代基取代、公开了 R¹ 和 R² 代表与相邻氮原子一起形成杂环的基团，L¹ 和 L² 各自代表卤素、烷基或烷氧基）及其盐、制备方法和含有这些化合物的药物组合物。这些化合物具有增加白细胞吞噬功能、增加巨噬细胞吞噬功能、恢复白细胞数量、激活感染保护功能、提高免疫能力、抗肿瘤等作用。 摘要 通式如下的新型融合吡唑化合物 其中所有符号如说明书中所定义，或其药学上可接受的盐，具有刺激白细胞吞噬作用、刺激巨噬细胞吞噬作用、恢复白细胞减少作用、刺激非特异性抗感染作用、抗肿瘤作用、激活免疫反应作用等，因此可用作药物。
• Pyridine compounds for treating amnesia
  申请人：YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

  公开号：EP0558094A1

  公开（公告）日：1993-09-01

  A novel compound of the formula wherein R¹ means hydrogen and R² means hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms; Ar means phenyl, a phenyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, amino, nitro and cyano, furyl, a furyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, thienyl, a thienyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, pyrrolyl, a pyrrolyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, pyridyl, or a pyridyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano: Y means a single bond or a straight-chain or branched chain alkylene having 1 to 8 carbon atoms which may have double bond(s) in the chain; W means a group of the formula (i) (wherein R³ and R⁴ are the same or different and respectively mean hydrogen or a halogen, X means -O- or -S-, Z means a single bond or -O-, A is a straight-chain or branched chain alkylene having 1 to 8 carbon atoms, B means -N(R⁸)(R⁹) (wherein R⁸ and R⁹ are the same or different and respectively mean hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms, or combinedly means a group forming, taken together with the adjacent nitrogen, 1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, piperidino, 1-piperazinyl, a 1-piperazinyl substituted by a straight-chain or branched chain alkyl having 1 to 8 carbon atoms at the 4-position, 1-homopiperazinyl, morpholino and thiomorpholino) or a group of the formula (ii) (wherein R¹² and R¹³ are the same or different and respectively mean hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms, P is -S- and Q is hexamethylene, heptamethylene, octamethylene, 1-methylpentamethylene, 1-methylhexamethylene, 1-methylheptamethylene, -(CH₂)₂S(CH₂)₃-, -(CH₂)₂S(CH₂)₆-. or a pharmaceutically acceptable salt thereof or a hydrate thereof. The compounds exhibit inhibitory activity on prolylendopeptidase. Also disclosed are pharmaceutical compositions containing the novel pyridine compounds.

  一种新颖的式化合物 其中 R¹ 指氢，R² 指氢或具有 1 至 8 个碳原子的直链或支链烷基；Ar 指苯基、被 1 至 3 个取代基取代的苯基，这些取代基选自卤素、具有 1 至 8 个碳原子的直链或支链烷基、具有 1 至 8 个碳原子的直链或支链烷氧基、三氟甲基、氨基、硝基和氰基、呋喃基、被 1 至 3 个取代基取代的呋喃基，这些取代基选自卤素、具有 1 至 8 个碳原子的直链或支链烷基、具有 1 至 8 个碳原子的直链或支链烷氧基、三氟甲基、具有 1 至 8 个碳原子的直链或支链烷硫基、具有 1 至 8 个碳原子的直链或支链烷基亚磺酰基、具有 1 至 8 个碳原子的直链或支链烷基磺酰基、氨基、硝基和氰基、噻吩基、被 1 至 3 个从卤素中选出的取代基取代的噻吩基、具有 1 至 8 个碳原子的直链或支链烷基、具有 1 至 8 个碳原子的直链或支链烷氧基、三氟甲基、具有 1 至 8 个碳原子的直链或支链烷硫基、具有 1 至 8 个碳原子的直链或支链烷基亚磺酰基、具有 1 至 8 个碳原子的直链或支链烷基磺酰基、氨基、硝基和氰基、吡咯基、被 1 至 3 个选自卤素的取代基取代的吡咯基、具有 1 至 8 个碳原子的直链或支链烷基、具有 1 至 8 个碳原子的直链或支链烷氧基、三氟甲基、具有 1 至 8 个碳原子的直链或支链烷硫基、具有 1 至 8 个碳原子的直链或支链烷基亚磺酰基、具有 1 至 8 个碳原子的直链或支链烷基磺酰基、氨基、硝基和氰基、吡啶基或被 1 至 3 个取代基取代的吡啶基，取代基可从卤素、具有 1 至 8 个碳原子的直链或支链烷基、具有 1 至 8 个碳原子的直链或支链烷氧基中选出、三氟甲基、1 至 8 个碳原子的直链或支链烷硫基、1 至 8 个碳原子的直链或支链 烷基亚磺酰基、1 至 8 个碳原子的直链或支链烷基磺酰基、氨基、硝基和氰基：Y 指单键或具有 1 至 8 个碳原子的直链或支链亚烷基，链中可能有双键； W 指式(i)的基团 (其中 R³ 和 R⁴ 相同或不同，分别指氢或卤素，X 指 -O- 或 -S-，Z 指单键或 -O-，A 指具有 1 至 8 个碳原子的直链或支链亚烷基，B 指 -N(R⁸)(R⁹)（其中 R⁸ 和 R𠞙 相同或不同，分别指氢或具有 1 至 8 个碳原子的直链或支链烷基、或组合指与邻近的氮一起形成的基团、1-吡咯烷基、2-氧代-1-吡咯烷基、哌啶基、1-哌嗪基、在 4 位上被具有 1 至 8 个碳原子的直链或支链烷基取代的 1-哌嗪基、1-高哌嗪基、吗啉基和硫代吗啉基）或式 (ii) 的基团 (其中 R¹² 和 R¹³ 相同或不同，分别指氢或具有 1 至 8 个碳原子的直链或支链烷基、P 是-S-，Q 是六亚甲基、七亚甲基、八亚甲基、1-甲基五亚甲基、1-甲基六亚甲基、1-甲基七亚甲基、-(CH₂)₂S(CH₂)₃-、-(CH₂)₂S(CH₂)₆-。 或 其药学上可接受的盐或其水合物。 这些化合物对原内酯肽酶具有抑制活性。还公开了含有新型吡啶化合物的药物组合物。
• Azine and Diazine Functionalization Using 2,2,6,6-Tetramethylpiperidino-Based Lithium–Metal Combinations: Application to the Synthesis of 5,9-Disubstituted Pyrido[3′,2′:4,5]pyrrolo[1,2-c]pyrimidines
  作者：Valérie Thiéry、Stéphane Bach、Florence Mongin、Nada Marquise、Tan Nguyen、Floris Chevallier、Laurent Picot、Olivier Lozach、Sandrine Ruchaud

  DOI：10.1055/s-0035-1560496

  日期：——

  The synthesis of triaryl methanols was investigated by reacting different 4-metalated 2-substituted pyrimidines with diaryl ketones, the latter being generated by deprotocupration-aroylation of azine and diazine substrates. Cyclization of the triaryl methanols thus obtained afforded pyrido[3,2:4,5]pyrrolo[1,2-c]pyrimidines, which were evaluated for kinase inhibition and antiproliferative activities in melanoma cells.