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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1061321Generated: October 31, 2026

Ethyl {[4-(4-oxo-1-piperidinyl)benzoyl]amino}acetate → Ethyl[(4-{4-[((2R)-2-hydroxy-2-[4-hydroxy-3-[(methylsulfonyl)amino]phenyl}ethyl)amino]-1-piperidinyl}benzoyl)amino]acetate

https://huagongshe.com/reaction/1061321

Reaction equation

Participants

RoleNameHCIDCharge
ReactantEthyl {[4-(4-oxo-1-piperidinyl)benzoyl]amino}acetateHCID 10733298—
Reactant(R)-N-(5-(2-amino-1-hydroxyethyl)-2-hydroxyphenyl)methanesulfonamideHCID 12047933—
ProductEthyl[(4-{4-[((2R)-2-hydroxy-2-[4-hydroxy-3-[(methylsulfonyl)amino]phenyl}ethyl)amino]-1-piperidinyl}benzoyl)amino]acetateHCID 10626150—

Reaction Steps

The title compound was prepared from ethyl {[4-(4-oxo-1-piperidineyl)benzoyl]amino}acetate (which was obtained in Example 161) and N-[5-((1R)-2-amino-1-hydroxy-ethyl)-2-hydroxy-phenyl]-methanesulfonamide (which was obtained in Example 10) according to the procedure of Example 180 as a white solid; mp >140° C. (decomposed); 1H NMR (300 MHz, DMSO-d6) δ 1.20 (t, J=7.1 Hz, 3H), 1.20-1.35 (m, 2H), 1.75-1.90 (m, 2H), 2.50-2.90 (m, 5 H), 2.90 (s, 3H), 3.70-3.85 (m, 2H), 3.93 (d, J=5.8 Hz, 2H), 4.10 (q, J=7.1 Hz, 2H), 4.47 (dd, J=7.9, 4.4 Hz, 1H), 6.79 (d, J=8.3 Hz, 1H), 6.90-7.00 (m, 3H), 7.16 (d, J=2.0 Hz, 1H), 7.72 (d, J=8.9 Hz, 2H), 8.58 (t, J=5.8 Hz, 1H); MS (ES) m/z: 535.2 (MH+); HRMS Calcd. for C26H37N4O7S(MH+): 535.2221. Found: 535.2216.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06525202B2
Source datasetuspto-grants-2003_02
ORD IDord-1121fe1e6c944b11b2a4f073c0c5aa90
Source noteuspto-grants-2003_02