RADIOSYNTHESIS OF [BENZOYL-3,4,5-H-3]DIFLUBENZURON BY A ROUTE APPLICABLE TO OTHER HIGH-POTENCY INSECT GROWTH-REGULATORS
RADIOSYNTHESIS OF [BENZOYL-3,4,5-H-3]DIFLUBENZURON BY A ROUTE APPLICABLE TO OTHER HIGH-POTENCY INSECT GROWTH-REGULATORS
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DOI：
10.1021/jf00079a045
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发表时间：
1988-01-01
影响因子：
6.1
通讯作者：
CASIDA, JE
中科院分区：
文献类型：
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作者：
TECLE, B;RUZO, LO;CASIDA, JE
由2，6-二氟苯甲酸和二溴异氰尿酸在浓硫酸中反应得到的2，6-二氟-3，4，5-三溴苯甲酸用于制备二氟三溴苯甲酰基类似物，其在催化还原脱溴作用下转化为相应的有效昆虫生长调节剂。通过制备60 Ci/mmol的[苯甲酰基-3，4，5 - 3 H]灭幼脲，说明了该反应顺序用于使用氚气的放射合成的适用性。
2,6-Difluoro-3,4,5-tribromobenzoic acid, from reaction of 2,6-difluorobenzoic acid and dibromoisocyanuric acid in concentrated sulfuric acid, is used to prepare difluorotribromobenzoyl analogues of diflubenzuron, chlorflurazuron, teflubenzuron, and XRD-473, which on catalytic reductive debromination are converted to the corresponding potent insect growth regulators. The applicability of this reaction sequence for radiosynthesis using tritium gas is illustrated by the preparation of [benzoyl-3,4,5-3H]diflubenzuron at 60 Ci/mmol.