摘要
目的探讨4-氯-2-氟-3-甲氧基苯硼酸的急性经口毒性、急性经皮毒性、急性皮肤刺激和急性眼刺激性。方法按照《化学品测试方法》(国家环境保护总局,2004年)开展急性经口毒性试验、急性经皮毒性试验、急性皮肤刺激试验和急性眼刺激性试验。结果 (1)急性经口毒性试验:雌性大鼠急性经口LD50为369 mg/kg,95%可信区间为227~599 mg/kg;雄性大鼠急性经口LD50为233 mg/kg,95%可信区间为160~399 mg/kg。对死亡大鼠解剖见肺脏充血。(2)急性经皮毒性试验:大鼠急性经皮LD50>2 500 mg/kg。(3)急性皮肤刺激试验:对大耳白兔染毒后各观察时点皮肤刺激反应总积分平均值和皮肤刺激反应时点最高积分均值均为0分。(4)急性眼刺激性试验:对大耳白兔眼刺激试验分级为5级。结论 4-氯-2-氟-3-甲氧基苯硼酸对雌雄性大鼠急性经口毒性分别属"低毒"、"中毒"。靶器官可能是肺脏;对大鼠急性经皮毒性属"实际无毒";对大耳白兔皮肤不产生刺激性,但可对眼睛产生中等刺激性。
Objective To study the acute oral toxicity,acute dermal toxicity,acute dermal irritation and acute eye irritation of4- chlorine- 2- fluoro- 3- methoxybenzeneboronic acid. Methods Tests for acute oral toxicity,acute dermal toxicity,acute dermal irritation and acute eye irritation of 4- chlorine- 2- fluoro- 3- methoxybenzeneboronic acid were conducted in compliance with the Guidelines for the Testing of Chemicals( State Environmental Protection Administration,2004). Results Acute oral toxicity test showed that the oral LD50 in female and male rats was 369 mg / kg( 95% CI: 227- 599 mg / kg) and 233 mg /kg( 95% CI: 160- 399 mg / kg) respectively. Pulmonary congestion in the dead rats was observed by anatomy.Acute dermal toxicity test showed that the dermal LD50 in rats was higher than 2,500 mg / kg. Acute dermal irritation test showed that the mean value of the total integral for each observation point after acute dermal exposure,and the highest integral recorded for all observation points were"0". Acute eye irritation test showed that the eye irritation was classified into Grade 5. Conclusions Acute oral toxicity of 4- chloro- 2- fluoro- 3- methoxybenzeneboronic acid for female and male rats belongs to low toxicity and moderate toxicity respectively. Lung may be the target organ. Acute dermal toxicity for rats is classified into practical non-toxic. It is not a dermal irritant to albino rabbits,but may be a medium ocular irritant.
引文
[1]国家环境保护总局.化学品测试方法[M].北京:中国环境科学出版社,2004:1-4.
[2]国家环境保护总局.HJ/T 154-2004新化学物质危害评估导则[S].北京:中国环境科学出版社,2004.
[3]钟为慧,叶海伟,刘振玉,等.含氟苯硼酸的合成及应用研究进展[J].有机化学,2009,29(5):665-671.
[4]徐丹,褚良银.苯硼酸及其衍生物在医药与化工领域的应用研究进展[J].化工进展,2006,25(9):1045-1048.
[5]周博.新型4-苯胺喹唑啉类分子靶向抗癌药物的制备及其微胶囊化研究[D].广州:华南理工大学,2012.
[6]赵昊昱.5-氟-2-甲氧基苯硼酸的合成[J].化学试剂,2013,35(2):178-182.
[7]王璐璐.通过SUZUKI偶联反应合成均三嗪类化合物[D].大连:大连理工大学,2012.
[8]董传华.芳基硼酸碘化反应的研究[D].洛阳:河南科技大学,2012.
