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CAS 1418130-40-1
2-Fluoro-6-aminophenylboronic acid pinacol ester
登记编号:(XI)1114845-1-a、(IV)1114845-2-a
应用背景(按来源药适应症)
非小细胞肺癌格索雷塞结直肠癌格索雷塞实体瘤格索雷塞肾细胞癌格索雷塞胰腺癌格索雷塞
来源药(使用该中间体的合成路线)
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 格索雷塞Garsorasib | Tier C · 观察 / 贸易 | - |
合成路线中的位置(上下游链)
按路线登记顺序排列,左→右为合成方向;高亮为当前 CAS,其余可点击跳转对应档案。
2,6-Bis(chloranyl)-5-fluoranylpyridine-3-carboxylic acid→2,6-Dichloro-5-fluoronicotinamide→2-Chloro-2-oxoacetyl chloride→4,6-Dicyclopropylpyrimidin-5-amine→4,6-Dichloropyrimidin-5-amine→(Cyclopropyl)boronic acid→2,6-Dichloro-N-[(4,6-dicyclopropylpyrimidin-5-yl)carbamoyl]-5-fluoropyridine-3-carboxamide→7-Chloro-1-(4,6-dicyclopropylpyrimidin-5-yl)-6-fluoropyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione→Trifluoroacetic acid 1-[(2R,5S)-2,5-dimethylpiperazin-1-yl]prop-2-en-1-one→7-Chloro-1-(4,6-dicyclopropylpyrimidin-5-yl)-4-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-6-fluoropyrido[2,3-d]pyrimidin-2(1H)-one→2-Fluoro-6-aminophenylboronic acid pinacol ester→tert-Butyl (2S,5R)-2,5-dimethylpiperazine-1-carboxylate→2-Propenoyl chloride→tert-Butyl (2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazine-1-carboxylate
7-Chloro-1-(4,6-dicyclopropylpyrimidin-5-yl)-6-fluoropyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione→(2R,5S)-1-Boc-2,5-dimethylpiperazine→tert-Butyl (2R,5S)-4-[7-chloro-1-(4,6-dicyclopropylpyrimidin-5-yl)-6-fluoro-2-oxo-1,2-dihydropyrido[2,3-d]pyrimidin-4-yl]-2,5-dimethylpiperazine-1-carboxylate→2-Fluoro-6-aminophenylboronic acid pinacol ester→tert-Butyl (2R,5S)-4-[7-(2-amino-6-fluorophenyl)-1-(4,6-dicyclopropylpyrimidin-5-yl)-6-fluoro-2-oxo-1,2-dihydropyrido[2,3-d]pyrimidin-4-yl]-2,5-dimethylpiperazine-1-carboxylate→7-(2-Amino-6-fluorophenyl)-1-(4,6-dicyclopropylpyrimidin-5-yl)-4-[(2S,5R)-2,5-dimethylpiperazin-1-yl]-6-fluoropyrido[2,3-d]pyrimidin-2(1H)-one→(Chloromethyl)acetyl chloride→7-(2-Amino-6-fluorophenyl)-4-[(2S,5R)-4-(3-chloropropanoyl)-2,5-dimethylpiperazin-1-yl]-1-(4,6-dicyclopropylpyrimidin-5-yl)-6-fluoropyrido[2,3-d]pyrimidin-2(1H)-one
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