摘要
对氟苯胺在盐酸的作用下与硫氰酸铵反应得到对氟苯基硫脲,然后在溴的作用下环化得到2-氨基-6-氟苯并噻唑;2-氨基-6-氟苯并噻唑水解并与氯化锌反应得2-氨基-5-氟苯硫酚锌盐;2-氨基-5-氟苯硫酚锌盐与D-丙氨酸-N-羰酐反应得到(R)-1-(6-氟-2-苯噻唑)乙胺。最后,(R)-1-(6-氟-2-苯噻唑)乙胺与L-缬氨酸和氯甲酸异丙酯反应得到目的产物苯噻菌胺,总收率51.2%(以对氟苯胺计)。
P-fluoroaniline reacted with ammonium thiocyanate in the present of hydrochloric acid to give 4-fluoro-phenylthioureas, then 4-fluoro-phenylthioureas reacted with bromine in the solution of chloroform to give the 2-amino-6-fluorol-benzothiazoles. In the present of NaOH, 2-amino-6-fluorol-benzothiazoles hydrolyzed and reacted with ZnCl2 to give the bis(5-fluoro-2-aminothiophenol) zinc salt. (R)-1-(6-fluoro-2-benzothiazoly)ethylamine was prepared by the reaction of bis(5-fluoro-2-aminothiophenol) zinc salt with D-alanine-N-carboxy anhydride. Under the catalytic of NaOH, (R)-1-(6-fluoro-2-benzothiazoly) ethylamine reacted with L-valine and isopropyl chlorocarbonate to give the target production of benthiavalicarb. The total yield is 51.2%(calculation on p-fluoroaniline).
出处
《世界农药》
CAS
2014年第5期34-36,共3页
World Pesticide
关键词
杀菌剂
苯噻菌胺
合成
fungicides
benthiavalicarb
synthesis