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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 434066Generated: October 30, 2026

Benzoic Acid → (2S,3R)-N-tert-Butoxycarbonyl-3-benzoyloxy-2-pyrrolidinecarboxylic acid methyl ester

https://huagongshe.com/reaction/434066

Reaction equation

Participants

RoleNameHCIDCharge
ReactantBenzoic AcidHCID 243—
ReactantTriphenylphosphineHCID 11776—
ReactantDiethyl azodicarboxylateHCID 5462977—
Reactant1-tert-butyl 2-methyl (2S,3S)-3-hydroxypyrrolidine-1,2-dicarboxylateHCID 14729253—
SolventTetrahydrofuranHCID 8028—
Product(2S,3R)-N-tert-Butoxycarbonyl-3-benzoyloxy-2-pyrrolidinecarboxylic acid methyl esterHCID 5858361894.2%

Reaction Steps

To a solution of 7A (13.5 g, 55 mmol) in anhydrous THF (500 mL) was added triphenylphosphine (26 g, 99 mmol), followed by benzoic acid (10.1 g, 82.7 mmol) and DEAD (9.5 mL, 60 mmol). The reaction mixture was stirred at RT for 2 hours, then partitioned between water and CH2Cl2. The organic phase was washed with saturated aqueous NaHCO3 and brine, dried over Na2SO4 and filtered. The filtrate was concentrated under reduced pressure to give a crude product, which was chromatographed (silica gel) eluting with 15% EtOAc/hexane to give 18.1 g of the title compound as a colorless oil.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06670386B2
Source datasetuspto-grants-2003_12
ORD IDord-d12d536c3fcc499783346596473c3aa3
Source noteuspto-grants-2003_12