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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 74931Generated: October 26, 2026

Methyl chloroformate → methyl (1S,2S)-2-(2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)cyclohexylcarbamate

https://huagongshe.com/reaction/74931

Reaction equation

Participants

RoleNameHCIDCharge
ReactantMethyl chloroformateHCID 6586—
ReactantDiisopropylethylamineHCID 81531—
Reactant(1S,2S)-N-[2-[5-chloro-1-(p-tolylsulfonyl)pyrrolo[5,4-b]pyridin-3-yl]-5-fluoro-pyrimidin-4-yl]cyclohexane-1,2-diamineHCID 68007676—
SolventDichloromethaneHCID 6344—
SolventEthyl AcetateHCID 8857—
Productmethyl (1S,2S)-2-(2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)cyclohexylcarbamateHCID 68101595—

Reaction Steps

To a mixture of (1S,2S)—N1-(2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-yl)cyclohexane-1,2-diamine, 23b, (0.18 g, 0.35 mmol) in dichloromethane (4 mL) at room temperature was added iPr2NEt (0.12 mL, 0.70 mmol) followed by methyl chloroformate (0.03 mL, 0.37 mmol). After 35 minutes. the mixture was diluted with EtOAc, washed successively with aqueous saturated NH4Cl and aqueous saturated NaHCO3 and brine, dried over Na2SO4 filtered and concentrated in vacuo to provide the crude product sufficiently pure for use in the next reaction.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08829007B2
Source datasetuspto-grants-2014_09
ORD IDord-636abb91438d4da08f88e8b06429aa83
Source noteuspto-grants-2014_09