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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1004819Generated: October 31, 2026

Methyl chloroformate → (S)-(-)-4-[4-[5-[(Acetylamino)methyl]-2-oxo-3-oxazolidinyl]-2-fluorophenyl]-1-piperidinecarboxylic acid methyl ester

https://huagongshe.com/reaction/1004819

Reaction equation

Participants

RoleNameHCIDCharge
ReactantMethyl chloroformateHCID 6586—
ReactantSodium BicarbonateHCID 516892—
Reactant(S)-(-)-N-[[2-Oxo-3-[4-(4-piperidinyl)-3-fluorophenyl]-5-oxazolidinyl]methyl]acetamideHCID 15887422—
SolventTetrahydrofuranHCID 8028—
SolventEthyl AcetateHCID 8857—
Product(S)-(-)-4-[4-[5-[(Acetylamino)methyl]-2-oxo-3-oxazolidinyl]-2-fluorophenyl]-1-piperidinecarboxylic acid methyl esterHCID 54000735—

Reaction Conditions

Temperature0 °C

Reaction Steps

A mixture of (S)-(-)-N-[[2-oxo-3-[4-(4-piperidinyl)-3-fluorophenyl]-5-oxazolidinyl]methyl]acetamide (EXAMPLE 20, 150 mg) and sodium bicarbonate (75 mg) in dry tetrahydrofuran (6 mL) at 0° C. under N2 is treated with methyl chloroformate (38 μL), and the resulting mixture is stirred at 0° C. for one hour. The reaction is then diluted with ethyl acetate (20 mL), washed with water (10 mL) and saline (10 mL), dried over anhydrous magnesium sulfate and concentrated under reduced pressure, and the residue is recrystallized from methylene chloride/diethyl ether to give the title compound, mp 165-166° C.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06051716
Source datasetuspto-grants-2000_04
ORD IDord-df6fedfb99104101bfeb90f8c642c2da
Source noteuspto-grants-2000_04