CN1115959C - 提高防治螨害持效性的方法 - Google Patents
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Abstract
本发明提供了一种提高防治螨害持效性的方法，即通过对植物的枝叶使用如结构式I所示的非对称4，6-二(芳氧基)嘧啶化合物。
Description
螨虫在园艺植物和农作物方面都造成了巨大的经济损失。具体地说，螨虫侵噬植株的枝叶和成熟中的果实，由此毁坏了柑橘类和梨果类的果实。
为了控制螨害，需要在生长季节用市售的杀螨剂对植株处理多次。尽管可以多次使用目前市售的杀螨剂，但是螨害仍然会对植株造成损害。所以，人们一直在研究开发新的、更有效的杀螨剂，它不需要多次使用就能够保护植株免受螨害。
WO94/02470中描述了可以用作杀螨剂的某些嘧啶化合物。但是，其中没有公开任何持效杀螨活性。
所以，本发明的目的是提供提高防治螨害持效性的方法。
后文详细的描述将清楚的说明本发明的以上及其它目的。
本发明提供了提高防治螨害持效性的方法，即通过向对螨害敏感的植物的枝叶使用杀螨有效量的非对称4，6-二(芳氧基)嘧啶化合物。
本发明提供了一种提高防治螨害持效性的方法，即通过向对螨害敏感的植物的枝叶使用杀螨有效量的如结构式I所示的非对称4，6-二(芳氧基)嘧啶化合物。其中，X是Cl、硝基或氰基。
WO94/02470中对本发明的非对称4，6-二(芳氧基)嘧啶化合物及其相应的对称类似物有所描述。其中只说明了急性(非持效性)杀螨评价。出人意料的是，现在发现，在对植株的枝叶使用生物对等急性剂量(即LC99值)的嘧啶化合物时，就持效防螨而言，本发明的非对称4，6-二(芳氧基)嘧啶化合物比其对应的对称嘧啶化合物有效得多。
通过一次性使用本发明的非对称4，6-二(芳氧基)嘧啶化合物就可以获得免受螨害的全季节保护作用，这是十分有利的。通过一次性使用本发明的非对称4，6-二(芳氧基)嘧啶化合物获得免受螨害的全季节保护作用显著减轻了因使用常规杀螨剂对环境造成的负担，常规杀螨剂要保护植株免受螨害需要使用多次。
在本发明的优选实施例之一中，非对称4，6-二(芳氧基)嘧啶化合物是4-[(4-氯-α，α，α-三氟-间-甲苯基)氧]-6-[(α，α，α，4-四氟-间-甲苯基)氧]嘧啶。
本发明结构式I所示的化合物对持效控制以下及其它食植物螨虫尤其有效：叶螨科，例如普通红叶螨，太平洋红叶螨，神泽叶螨，榆苹全爪螨，桔全爪螨和草地小爪螨；趺线螨科，例如Phytonemus pallidus和侧多食趺线螨；瘿螨科，例如苹次瘿螨，桔锈瘿螨和桔芽瘤瘿螨；细须螨科，例如紫红短须螨本发明的非对称4，6-二(芳氧基)嘧啶化合物对持效防治普通红叶螨，榆苹全爪螨，桔全爪螨和紫红短须螨尤其有效。
利用本发明结构式I所示化合物可以获得长期抗螨害保护的植物包括但不限于柑橘类，例如橙、葡萄柚、柠檬和酸橙；梨果类，例如苹果、梨和猕猴桃；核果，例如油梨、桃子、樱桃、无花果、橄榄和芒果；蔓生水果，例如葡萄、草莓和覆盆子；坚果，例如杏仁、核桃、胡桃、阿月浑子果、腰果、榛子、栗子、马卡达姆坚果和巴西坚果(Brazil nut)；农田作物，例如棉花、玉米、大豆、小麦、南瓜和西瓜；观赏植物，例如开花植物和灌木；咖啡和茶叶。本发明非对称4，6-二(芳氧基)嘧啶化合物对长期保护柑橘类植物和梨果类水果免受螨害尤其有效。
为了长期控制螨害，通常用约含1g/百升(hl)至100g/hl，5g/hl至25g/hl更好的结构式I所示非对称4，6-二(芳氧基)嘧啶化合物的液体(最好是水)分散系来处理果树和观赏植物。实际操作中，分散系通常施用于果树或观赏植物直至流滴。
在将本发明的非对称4 ，6-二(芳氧基)嘧啶化合物足量用于农田作物时，即达到约0.01kg/ha至1.0kg/ha的活性成份，约0.081kg/ha至0.3kg/ha更好，它也能够延长对螨害的持效控制。
本文的“枝叶”包括但不限于植株的叶子、叶芽、果实、茎、小枝、大枝和/或花。“果树”包括但不限于柑橘类、梨果类、核果类、蔓生类和坚果类。“观赏植物”包括但不限于开花植物和灌木。“农田作物”包括但不限于南瓜和西瓜之类的蔬菜，以及棉花、玉米、大豆和小麦之类的成行种植的农作物。
本发明的非对称4，6-二(芳氧基)嘧啶化合物可以被配制成可乳化浓缩液、流动性浓缩液或可湿性粉末，它们可以用水或其它合适的极性溶剂稀释，通常是就地稀释，然后以稀释喷剂的形式使用。本发明的非对称4，6-二(芳氧基)嘧啶化合物还可以配制成无水压缩颗粒，颗粒制剂，粉尘制剂，粉尘浓缩物，悬浮浓缩液，微乳液等。这类制剂或组合物中含有本发明的某种非对称4，6-二(芳氧基)嘧啶化合物(或此类化合物的混合物)，并混以一种或多种农艺学上可接受的惰性、固体或液体载体。
为了便于理解本发明，以下实施例主要是为了更详细的说明本发明。本发明的范围不应理解为实施例所限，它包括了权利要求中所限定的全部主题。
实施例1
对温室条件下抗普通红叶螨的持效杀螨活性的评价
将棉豆(sieva lima bean)的叶浸在50％的丙酮测试溶液中。每份测试溶液中含有两倍于普通红叶螨LC99值的待评价化合物。使用的LC99值是在急性剂量评价中杀死99％普通红叶螨的化合物ppm浓度。因为使用LC99值，在评价一开始使用的是生物对等急性剂量的测试化合物。然后令植株吹干，植于苗床，下灌溉，放在温室内，每天光照14小时。然后在处理后的第0、3和7天对植株进行次级取样。在每一取样时段，将该植株移出温室，每片叶接受约50至60个普通红叶螨的侵害。3天后，计数成年螨的个数并估计螨虫的死亡率。结果列于表I。
评价化合物是如下表示的。表I中是使用以化合物数字编号表示的本发明化合物和以化合物字母编号表示的比较化合物获得的数据。
化合物
结构式
化学名称本发明化合物1
4-[(4-氯-α ，α，α-三氟-间-甲苯基)氧]-6-[(α，α，α，4-四氟-间-甲苯基)氧]嘧啶本发明化合物2
4-[(α，α，α，4-四氟-间-甲苯基)氧]-6-[(α，α，α-三氟-4-硝基-间-甲苯基)氧]嘧啶对称化合物A
4，6-二[(α，α，α，4-四氟-间-甲苯基)氧]嘧啶对称化合物B
4，6-二[(4-氯-α，α，α-三氟-间-甲苯基)氧]嘧啶
由表I的数据可以看出，本发明的非对称4，6-二(芳氧基)嘧啶化合物对于持效控制普通红叶螨明显比对应的对称类似物更为有效。因为在开始时对植株使用的是生物对等急性剂量，所以这一结果是出人意料的。
表I
嘧啶化合物的持效活性
比例 普通红叶螨死亡率％
2X-LC99 处理后的天数
化合物
(ppm)
0
3
7本发明化合物1 7 100 99 99本发明化合物2 10 100 96 97对称化合物A 8 100 80 25对称化合物B 6 100 49 未评价
实施例2
对持效杀螨活性的实地评价
用手持式喷雾器以约1,000至2,000l/ha的喷雾体积对植株的枝叶施用含5或15g/hl测试化合物的水性混合物(即施用至流滴)，由此实地评价对乔木水果和柑橘类的几种食植物螨虫的持效控制作用。水性混合物是通过在水中加入适量测试化合物的可乳化浓缩液制备的。在该项评价中，可乳化浓缩液含有9.7wt/wt％测试化合物，3.5wt/wt％TOXIMUL3403F(一种阴离子/非离子除垢剂混合物，购自Stepan Company，Northfield，Illinois)，3.5wt/wt％TOXIMUL3404F(一种阴离子/非离子除垢剂混合物，购自Stepan Company)，和83.3wt/wt％AROMATIC200(一种芳香烃溶剂混合物，购自EXXON Chemicals Americas，Houston，Texas)。
用药后，每周观察植株上是否有活螨。然后将处理过的植株上的螨虫数量与未处理的植株上的螨虫数量比较，由此评价测试化合物的持效活性。评价结果列于表II至表VI。表II至表VI中的化合物以实施例1中的数字和字母编号表示。
从表II至表VI中的数据可以看出，本发明的非对称4，6-二(芳氧基)嘧啶化合物(4-[(4-氯-α，α，α-三氟-间-甲苯基)氧]-6-[(α，α，α，4-四氟-间-甲苯基)氧]嘧啶)对于持效控制麻风性螨虫(leprosis mite)、红螨和欧洲红螨比对称的嘧啶类似物(4，6-二[(α，α，α，4-四氟-间-甲苯基)氧]嘧啶)有效得多。
表II
对桔树上的紫红短须螨实地使用嘧啶化合物后的评价-评价1
螨虫控制百分率
比例 处理后的天数
化合物
(g/hl)
7
28
50
63本发明化合物1 15 94 100 90 100
5 100 100 93 88对称化合物A 15 97 100 93 88
5 94 100 69 68
表III
对桔树上的紫红短须螨实地使用嘧啶化合物后的评价-评价2
螨虫控制百分率
比例 处理后的天数
化合物
(g/hl)
7
30
70
90
120本发明化合物1 15 100 98 98 94 99
5 100 94 96 91 79对称化合物A 15 100 94 98 58 63
5 100 95 89 58 64
表IV
对桔树上的紫红短须螨实地使用嘧啶化合物后的评价-评价3
螨虫控制百分率
比例 处理后的天数
化合物
(g/hl)
7
35
60
90
124本发明化合物1 15 89 100 100 100 98
95 100 98 98 80对称化合物A 15 97 100 100 98 71
96 94 95 72 0
表V
对桔树上的桔全爪螨实地使用嘧啶化合物后的评价
螨虫控制百分率
比例 处理后的天数
化合物
(g/hl)
7
21
30本发明化合物1 15 99 97 94对称化合物A 15 88 85 69
表VI
对苹果上的榆苹全爪螨实地使用嘧啶化合物后的评价
螨虫控制百分率
比例 处理后的天数
化合物
(g/hl)
2
14
21
36本发明化合物1 15 97 99 97 94
5 77 92 94 64对称化合物A 15 90 93 96 78
5 77 70 86 28
Claims (6)
1.一种提高防治螨害持效性的方法，它包括对易患螨害的植物的枝叶使用杀螨有效量的具有如下结构式的非对称4，6-二(芳氧基)嘧啶化合物，
其中的X是Cl，硝基或氰基。
2.根据权利要求1所述的方法，其中的化合物是4-[(4-氯-α，α，α-三氟-间-甲苯基)氧]-6-[(α，α，α，4-四氟-间-甲苯基)氧]嘧啶。
3.根据权利要求1所述的方法，其中的植物选自柑橘类、梨果类、核果类、蔓生果类、坚果类、农田作物、观赏植物、咖啡和茶叶。
4.根据权利要求1所述的方法，其中的植物是果树或观赏植物，该化合物施用于植物的枝叶的比例是1g/hl至100g/hl。
5.根据权利要求1所述的方法，其中的植物是农田作物，该化合物施用于植物的枝叶的比例是0.01kg/ha至1.0kg/ha。
6.根据权利要求1所述的方法，其中的螨虫选自普通红螨、榆苹全爪螨、桔全爪螨和紫红短须螨。
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| US08/874,116 US5883104A (en) | 1997-06-12 | 1997-06-12 | Methods for improving the residual control of mites and prolonging the protection of plants from mites infestations |
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| DE10055941A1 (de) | 2000-11-10 | 2002-05-23 | Bayer Ag | Wirkstoffkombinationen mit insektiziden und akariziden Eigenschaften |
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