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CAS 1418130-40-1

2-Fluoro-6-aminophenylboronic acid pinacol ester

Codes: (XI)1114845-1-a, (IV)1114845-2-a

Application context (from source-drug indications)

Non-small cell lung cancerGarsorasibColorectal cancerGarsorasibSolid tumourGarsorasibRenal cell carcinomaGarsorasibPancreatic cancerGarsorasib

Source drugs (routes using this intermediate)

DrugTierExpiry
GarsorasibTier C — Watch / trade-

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

GarsorasibOptimised routesteps: 5total yield: /
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
GarsorasibOptimised routesteps: 5total yield: /
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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