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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 8471Generated: October 23, 2026

Diethyl (ethoxymethylene)malonate → Diethyl [2,3,4-trifluoro[(1S)-2-hydroxy-1-methylethyl]anilino]methylenemalonate

https://huagongshe.com/en/reaction/8471

Reaction equation

Participants

RoleNameHCIDCharge
ReactantDiethyl (ethoxymethylene)malonateHCID 6871—
Reactant(2S)-2-(2,3,4-Trifluoroanilino)propanolHCID 11401466—
ProductDiethyl [2,3,4-trifluoro[(1S)-2-hydroxy-1-methylethyl]anilino]methylenemalonateHCID 1148565278%

Reaction Conditions

Temperature100 °C

Reaction Steps

To the compound (103 mg) obtained in Example 51 was added diethyl ethoxymethylenemalonate (127 mg). Then the obtained mixture was stirred for 1 hour while heating to 100° C. under atmospheric pressure. Further, it was stirred at the same temperature for 1.5 hour under reduced pressure and then under atmospheric pressure for additional 16 hours. By analyzing reversed phase HPLC with the use of the compound of Example 63 as a specimen, the obtained product corresponded to 142 mg (78%) of the title compound.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07087778B2
Source datasetuspto-grants-2006_08
ORD IDord-426f633887724b84bb4638f94290938a
Source noteuspto-grants-2006_08