avermectin A_2a | 65195-53-1

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酯类和类似物
• 英文名称: avermectin A_2a
• 英文别名: Avermectin A2a；(1R,4S,4'S,5'S,6R,6'R,8R,10E,12S,13S,14E,16E,20R,21R,24S)-6'-butan-2-yl-4',24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-21-methoxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
• CAS: 65195-53-1
• 化学式: C₄₉H₇₆O₁₅
• 分子量: 905.133
• InChiKey: JVGWUGTWQIAGHJ-DFAYUBCLSA-N

物化性质

• 沸点：
  952.2±65.0 °C(Predicted)
• 密度：
  1.23±0.1 g/cm3(Predicted)
• 溶解度：
  可溶于DMSO（少许）、甲醇（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  64
• 可旋转键数：
  9
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  179
• 氢给体数：
  3
• 氢受体数：
  15

反应信息

• 作为反应物：
  描述：

  avermectin A_2a 在 硫酸 作用下， 以 异丙醇 为溶剂， 反应 16.0h， 以87%的产率得到deoleandro-avermectin A2A
  参考文献：
  名称：

  Avermectin aglycons

  摘要：

  DOI：

  10.1021/jo00342a023

文献信息

• DIMERIC AVERMECTIN AND MILBEMYCIN DERIVATIVES
  申请人：Meng Charles Q.

  公开号：US20100144859A1

  公开（公告）日：2010-06-10

  This invention provides for novel antiparasitic and pesticidal derivatives of avermectin and milbemycin compounds in which two avermectin or milbemycin members are linked together by a chemical linker. The resulting compounds may be used in veterinary compositions which are used in treating, controlling and preventing of endo- and ectoparasite infections and infestations in animals or for combating pests in plants or plant propagation material.

  这项发明提供了一种新颖的阿维菌素和米氏菌素衍生物，其中两个阿维菌素或米氏菌素成员通过化学连接剂连接在一起。所得的化合物可用于兽药组合物中，用于治疗、控制和预防动物体内和体外寄生虫感染及寄生虫侵染，或用于对抗植物或植物繁殖材料中的害虫。
• AVERMECTIN DERIVATIVES
  申请人：Jeschke Peter

  公开号：US20100234312A1

  公开（公告）日：2010-09-16

  Novel avermectin derivatives of the formula (I) in which —C 22 R 1 -A-C 23 R 2 , R 3 , R 4 and R 5 have the meanings given in the description, processes for preparing these compounds and their use for controlling animal pests, and also novel intermediates and their preparation

  本发明涉及一种新的阿维菌素衍生物，其化学式为（I），其中—C22R1-A-C23R2，R3，R4和R5的含义如描述所述，本发明还涉及制备这些化合物的方法、用于控制动物害虫的方法，以及新的中间体及其制备方法。
• Synergistic Combination of Glutamate-and Gaba-Gated Chloride Agonist Pesticide and at Least One Vitamin E, Niacin, or Derivatives Thereof
  申请人：Pedersen Morten

  公开号：US20090111759A1

  公开（公告）日：2009-04-30

  Presented are pesticidal compositions comprising at least one pesticide selected among Glutamate- or GABA-gated chloride channel agonist pesticides and at least one synergist which is selected among Vitamin E, Niacin and derivatives thereof. The combinations of these compounds show a synergistic effect allowing a composition to be prepared comprising a lesser amount of pesticide, while still controlling the harmful pests.

  提供的是杀虫组合物，包括至少一种从谷氨酸或GABA门控氯离子通道激动剂杀虫剂中选择的杀虫剂，以及至少一种从维生素E、烟酸及其衍生物中选择的协同剂。这些化合物的组合表现出协同效应，允许制备含较少杀虫剂的组合物，同时仍然控制有害的害虫。
• Avermectin epoxide derivatives
  申请人：Merck & Co., Inc.

  公开号：EP0136892A2

  公开（公告）日：1985-04-10

  Novel avermectin epoxides have the formula: in which the broken line at the 22,23-position indicates a single or a double bond; R, is hydrogen or hydroxy and is present only when the broken line at the 22,23-position indicates a single bond; R1 is iso-propyl or sec-butyl; R3 is hydroxy or methoxy; R4 is hydroxy. a-L-oleandrosyloxy, or 4'-(a-L-oleandrosyl)-a-L-oleandrosyloxy; and the dotted triangular figures at the 8,9 and 14,15 positions indicate a double bond or an epoxide, provided that at least one of the 8,9 and 14,15 positions is epoxidized. The epoxides are prepared by oxidizing an avermectin compound with a mild oxidizing agent. The avermectin epoxide compounds have utility as anti-parasitic agents and can be made into compositions suitable for that use. The compounds are also highly potent insecticides against agricultural pests.

  新型阿维菌素环氧化物的化学式为 其中，22,23-位的折线表示单键或双键；R, 是氢或羟基，仅当 22,23- 位的折线表示单键时才存在；R1 是异丙基或仲丁基；R3 是羟基或甲氧基；R4 是羟基。在 8、9 和 14、15 位置上的三角形虚线表示双键或环氧化物，条件是 8、9 和 14、15 位置上至少有一个位置被环氧化。环氧化物的制备方法是用温和的氧化剂氧化阿维菌素化合物。阿维菌素环氧化物化合物可用作抗寄生虫药剂，并可制成适用于该用途的组合物。这些化合物也是防治农业害虫的高效杀虫剂。
• Reduced avermectin derivatives
  申请人：Merck & Co., Inc.

  公开号：EP0266131A1

  公开（公告）日：1988-05-04

  There are disclosed novel avermectin reduction products. The compounds are prepared by selective catalytic hydrogenation of avermectin-like compounds or by reaction of selected double bonds with electrophylic reagents. The reduced avermectin compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests. The reduced, avermectin compounds have increased stability towards light which prolongs their insecticidal activities when applied to field crops subject to irradiation by sunlight.

  本发明公开了新型阿维菌素还原产物，这些化合物是通过阿维菌素类化合物的选择性催化氢化反应或通过选定的双键与电解试剂反应制备的。 还原阿维菌素化合物可用作抗寄生虫药剂，本发明还公开了用于该用途的组合物，这些化合物也是针对农业害虫的高效杀虫剂。 还原阿维菌素化合物对光的稳定性增强，当应用于受阳光照射的田间作物时，可延长其杀虫活性。