新型除草剂丙酯草醚的微量合成

MICROSYNTHESIS OF A NOVEL HERBICIDE,PROPYL 4-[2-[(4,6-DIMETHOXY-2-PYRIMIDINYL)OXY] BENZYLAMINO]BENZOATE

从苯酚、对氨基苯甲酸和2-甲硫基-4,6-二氯嘧啶出发,建立了包含取代、氧化和缩合等7步反应的丙酯草醚除草剂微量制备方法。最终产物经制备HPLC纯化,其收率为53%,化学纯度大于98%,用MS(EI)、HPLC-MS1、H-NMR、UV等方法确认了丙酯草醚的结构。所建立的丙酯草醚微量制备方法,为放射性同位素标记丙酯草醚的合成奠定了基础。

ZJ273, propyl 4-[ 2-[ （4, 6-dimethoxy-2-pyrimidinyl） oxy ] benzylamino ] benzoate, is a novel herbicide. The microsynthetic method of the compound was developed from 4,6-dimethoxy-2-pyrimidine, propyl （4-benzylamino） benzoate and phenol, and then purified by preparative-HPLC. The yield of end product was 53 % . Its chemical structure was characterized by means of 1H-NMR, MS, UV, and its chemical purity was determined to be exceed 98 % by HPLC. The microsynthetic method of propyl 4-[2-[（4, 6-dimethoxy-2-pyrimidinyl）oxy] benzylamino] benzoate developed sets up a basis to synthesize the radioisotopic labeled target compound.