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CAS 1454847-97-2

(S)-1-(5-fluoro-2-iodophenyl)ethyl methanesulfonate

Codes:LORL-003

Application context (from source-drug indications)

非小细胞肺癌洛拉替尼

Source drugs (routes using this intermediate)

DrugTierExpiry
洛拉替尼LorlatinibTier B — Position early2030

Position in synthesis routes (up/downstream chain)

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洛拉替尼原研路线steps: 9total yield: 110 mg
1-(5-fluoro-2-iodophenyl)ethanone→(S)-1-(5-fluoro-2-iodophenyl)ethanol→(S)-1-(5-fluoro-2-iodophenyl)ethyl methanesulfonate→2-aminopyridin-3-ol→(R)-3-(1-(5-fluoro-2-iodophenyl)ethoxy)pyridin-2-amine→(R)-methyl 2-(1-((2-aminopyridin-3-yl)oxy)ethyl)-4-fluorobenzoate→(R)-methyl 2-(1-((2-amino-5-bromopyridin-3-yl)oxy)ethyl)-4-fluorobenzoate→tert-butyl ((4-bromo-5-cyano-1-methyl-1H-pyrazol-3-yl)methyl)(methyl)carbamate→(R)-methyl 2-(1-((2-amino-5-(3-(((tert-butoxycarbonyl)(methyl)amino)methyl)-5-cyano-1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)oxy)ethyl)-4-fluorobenzoate→(R)-2-(1-((2-amino-5-(3-(((tert-butoxycarbonyl)(methyl)amino)methyl)-5-cyano-1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)oxy)ethyl)-4-fluorobenzoic acid→(R)-2-(1-((2-amino-5-(5-cyano-1-methyl-3-((methylamino)methyl)-1H-pyrazol-4-yl)pyridin-3-yl)oxy)ethyl)-4-fluorobenzoic acid hydrochloride

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