吡利霉素盐酸盐 | 78822-40-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 吡利霉素盐酸盐
• 中文别名: 吡利霉素盐酸化物
• 英文名称: pirlimycin hydrochloride
• 英文别名: (2S,4R)-N-[(1S,2S)-2-chloro-1-[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-methylsulfanyloxan-2-yl]propyl]-4-ethylpiperidin-1-ium-2-carboxamide;chloride
• CAS: 78822-40-9
• 化学式: C₁₇H₃₁ClN₂O₅S*ClH
• 分子量: 447.423
• InChiKey: DPVJWUUBZWFDPG-XEDDUELXSA-N

物化性质

• 熔点：
  >198°C (dec.)
• 比旋光度：
  D25 +176° (US 4278789); D25 +181°
• 溶解度：
  甲醇（微溶）、水（微溶）

计算性质

• 辛醇/水分配系数(LogP)：
  0.47
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.94
• 拓扑面积：
  136
• 氢给体数：
  6
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  聚合甲醛 、 吡利霉素盐酸盐 在 platinum(IV) oxide 氢气 作用下， 以 乙醇 为溶剂， 25.0 ℃ 、344.73 kPa 条件下， 反应 18.0h， 生成 N-methylpyrlimycin hydrochloride
  参考文献：
  名称：

  克林霉素类似物的合成和抗菌活性：吡林霉素1,2，一种有效的抗菌剂。

  摘要：

  描述了一系列克林霉素类似物的制备，其中该分子的天然存在的五元环状氨基酸酰胺部分被四元，六元或七元环状氨基酸酰胺替代。最有趣的化合物是吡霉素（7e，U-57,930E），其中克林霉素的（2S-反式）-4-正丙基丙基部分被（2S-顺式）-4-乙基哌酰胺取代。这种结构修饰导致毒性，新陈代谢和抗菌效力的明显有利变化。尽管克林霉素和吡霉素的体外抗菌活性几乎相同，但当对实验感染金黄色葡萄球菌，化脓性链球菌，肺炎链球菌，脆弱型拟杆菌的小鼠给药时，后者的活性是克林霉素的2-20倍。和伯氏疟原虫。皮下和口服给药后，吡嗪霉素在大鼠和小鼠中被吸收。它很容易穿透小鼠中脆弱的B. gilgilis引起的脓肿，并被隔离在这些脓肿中。皮下注射200 mg / kg剂量后，至少6倍于所需抑制浓度的药物浓度维持6小时。总生物活性的尿排泄仅由完整的吡霉素组成，未检测到其他抗菌活性代谢物。吡美霉素在大鼠和小鼠的给药水平上耐受良好。皮下注射200

  DOI：

  10.1021/jm00368a020

文献信息

• ARYLOAZOL-2-YL CYANOETHYLAMINO COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF
  申请人：Soll Mark David

  公开号：US20140080862A1

  公开（公告）日：2014-03-20

  The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R 3 , R 4 , R 5 , R 6 , R 7 , P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.

  本发明涉及新颖的式(I)的芳基咪唑-2-基-氰基乙基氨基衍生物：其中R3、R4、R5、R6、R7、P、Q、V、W、X、Y、Z和a如描述中所定义，以及其组合物、制备方法以及它们作为杀虫剂的用途。
• 1-Aryl-5-alkyl pyrazole derivative compounds, processes of making and methods of using thereof
  申请人：Lee Ik Hyoung

  公开号：US20080031902A1

  公开（公告）日：2008-02-07

  Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R 1 is hydrogen, cyano, halogen, R 8 , formyl, —C(O)R 8 , —C(O)OR 8 , —C(O)NR 9 R 10 , or —C(S)NH 2 ; R 2 is R 2 or —S(O) m R 11 ; R 3 is methyl, ethyl or C 1 -C 4 haloalkyl; R 4 , R 5 and R 7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R 6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R 12 , —S(O) n R 12 or SF 5 ; Z is a nitrogen atom or C—R 13 ; R 8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R 9 is hydrogen, alkyl, haloalkyl or alkoxy; R 10 is hydrogen, alkyl, haloalkyl or alkoxy; R 11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R 12 is alkyl or haloalkyl; R 13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.

  提供了1-芳基-5-烷基吡唑化合物，化学式为(I)：其中：R1为氢、氰基、卤素、R8、甲酰基、—C(O)R8、—C(O)OR8、—C(O)NR9R10或—C(S)NH2；R2为R2或—S(O)mR11；R3为甲基、乙基或C1-C4卤代烷基；R4、R5和R7独立地为氢、卤素、烷基、卤代烷基、氰基或硝基；R6为卤素、烷基、卤代烷基、烷氧基、卤代烷氧基、氰基、硝基、—C(O)R12、—S(O)nR12或SF5；Z为氮原子或C—R13；R8为烷基、卤代烷基、环烷基或卤代环烷基；R9为氢、烷基、卤代烷基或烷氧基；R10为氢、烷基、卤代烷基或烷氧基；R11为烷基、卤代烷基、烯基、卤代烯基、炔基、卤代炔基或环烷基；R12为烷基或卤代烷基；R13为氢、卤素、氰基、硝基、烷基、卤代烷基、烷氧基或卤代烷氧基；m为0、1或2；n为0、1或2；或其盐，制备化合物(I)的方法以及这些化合物对外寄生虫、内寄生虫和害虫的用途。
• THIOAMIDE COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF
  申请人：Le Hir de Fallois Loic Patrick

  公开号：US20110190231A1

  公开（公告）日：2011-08-04

  The present invention relates to novel thioamide derivatives of formula (I) and formula (Ia): wherein, R 3 , R 4 , R 5 , R 6 , R 7 , P, Q, T, V, W, X, Y, Z, a, m and n are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.

  本发明涉及公式（I）和公式（Ia）的新型硫代酰胺衍生物：其中，R3、R4、R5、R6、R7、P、Q、T、V、W、X、Y、Z、a、m和n如说明书中所定义的，以及它们的组成物、制备过程和它们作为杀虫剂的用途。
• 1-ARYL-5-ALKYL PYRAZOLE DERIVATIVE COMPOUNDS, PROCESSES OF MAKING AND METHODS OF USING THEREOF
  申请人：Lee Hyoung Ik

  公开号：US20100249194A1

  公开（公告）日：2010-09-30

  Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R 1 is hydrogen, cyano, halogen, R 8 , formyl, —C(O)R 8 , —C(O)OR 8 , —C(O)NR 9 R 10 , or —C(S)NH 2 ; R 2 is R 8 or —S(O) m R 11 ; R 3 is methyl, ethyl or C 1 -C 4 haloalkyl; R 4 , R 5 and R 7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R 6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R 12 , —S(O) n R 12 or SF 5 ; Z is a nitrogen atom or C—R 13 ; R 8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R 9 is hydrogen, alkyl, haloalkyl or alkoxy; R 10 is hydrogen, alkyl, haloalkyl or alkoxy; R 11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R 12 is alkyl or haloalkyl; R 13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.

  提供的是1-芳基-5-烷基吡唑化合物，化学式（I）如下： 其中：R1为氢、氰基、卤素、R8、甲酰基、—C（O）R8、—C（O）OR8、—C（O）NR9R10或—C（S）NH2；R2为R8或—S（O）mR11；R3为甲基、乙基或C1-C4卤代烷基；R4、R5和R7独立地为氢、卤素、烷基、卤代烷基、氰基或硝基；R6为卤素、烷基、卤代烷基、烷氧基、卤代烷氧基、氰基、硝基、—C（O）R12、—S（O）nR12或SF5；Z为氮原子或C—R13；R8为烷基、卤代烷基、环烷基或卤代环烷基；R9为氢、烷基、卤代烷基或烷氧基；R10为氢、烷基、卤代烷基或烷氧基；R11为烷基、卤代烷基、烯基、卤代烯基、炔基、卤代炔基或环烷基；R12为烷基或卤代烷基；R13为氢、卤素、氰基、硝基、烷基、卤代烷基、烷氧基或卤代烷氧基；m为0、1或2；n为0、1或2；或其盐。制备式（I）化合物的方法以及这些化合物对外寄生虫、内寄生虫和害虫的用途。
• Aryloazol-2-yl cyanoethylamino compounds, method of making and method of using thereof
  申请人：Merial Limited

  公开号：EP2639228A2

  公开（公告）日：2013-09-18

  The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.

  本发明涉及式（I）的新型芳基唑-2-基-氰乙基氨基衍生物：其中 R3、R4、R5、R6、R7、P、Q、V、W、X、Y、Z 和 a 如描述中所定义；本发明还涉及其组合物、制备工艺及其作为农药的用途。