除草剂双氟磺草胺的合成

Synthesis of Florasulam

[方法]以2,4-二氯-5-氟嘧啶为起始原料,经醚化反应、肼化反应、环合反应、苄硫醚化反应、异构化反应、氯氧化反应和酰胺化反应合成双氟磺草胺。[结果]以2,4-二氯-5-氟嘧啶计,产品总收率达66.7%,含量达97%,产品结构经氢谱核磁分析验证。[结论]该方法具有工艺路线合理、反应条件温合、原料易得、产品质量好、收率高、成本低等特点,适合于工业化生产。

[Methods] Using 2,4-dichloro-5-fluoropyrimidine as starting material, florasulam was synthesized by etherification, hydrazine reaction, cyclization, benzyl sulfide reaction, isomerization, chlorine oxidation and amidation. [Results] The total yield was 66.7% based on 2,4-dichloro-5-fluoropyrimidine, and the purity was 97%. Their structures were confirmed by tH NMR. [Conclusions] The process has advantages of reasonable process, mild reaction conditions, easy availability of materials, high product quality, high yield and low cost, and is suitable for industrialized production.