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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1867937Generated: October 30, 2026

Water → Ethyl 1-(2,4-dimethoxybenzyl)-7-(2-hydroxymethylpiperidin-1-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylate

https://huagongshe.com/reaction/1867937

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
ReactantAcetonitrileHCID 6342—
ReactantDiisopropylethylamineHCID 81531—
ReactantPiperidin-1-ylmethanolHCID 446909—
ReactantEthyl 7-chloro-1-(2,4-dimethoxybenzyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylateHCID 13937202—
ProductEthyl 1-(2,4-dimethoxybenzyl)-7-(2-hydroxymethylpiperidin-1-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylateHCID 69030307—

Reaction Conditions

Temperature75 °C

Reaction Steps

A mixture of EXAMPLE 1B (2.15 g), piperidinylmethanol (890 mg) and diisopropylethylamine (2.5 mL) in acetonitrile (50 mL) at 25° C. was stirred for 24 hours, heated at 75° C. for 5 days, cooled, treated with water, and extracted with dichloromethane (200 mL). The extract was washed with water and 1M hydrochloric acid and concentrated.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07632946B2
Source datasetuspto-grants-2009_12
ORD IDord-be7ac9be88d94205aa7e39f7e88acfe6
Source noteuspto-grants-2009_12