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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1061310Generated: November 3, 2026

[4-(4-Oxo-piperidin-1-yl)-phenyl]-acetic acid → (4-{4-[2-Hydroxy-2-(4-hydroxy-3-methanesulfonylamino-phenyl)-ethylamino]-piperidin-1-yl}-phenyl)-acetic acid

https://huagongshe.com/reaction/1061310

Reaction equation

Participants

RoleNameHCIDCharge
Reactant[4-(4-Oxo-piperidin-1-yl)-phenyl]-acetic acidHCID 10657278—
Reactant(R)-N-(5-(2-amino-1-hydroxyethyl)-2-hydroxyphenyl)methanesulfonamideHCID 12047933—
Product(4-{4-[2-Hydroxy-2-(4-hydroxy-3-methanesulfonylamino-phenyl)-ethylamino]-piperidin-1-yl}-phenyl)-acetic acidHCID 10718924—

Reaction Steps

The title compound was prepared from [4-(4-oxo-piperidine-1-yl)-phenyl]-acetic acid (which was obtained in Example 149) and N-[5-(2-amino-(1 R)-1-hydroxy-ethyl)-2-hydroxy-phenyl]-methanesulfonamide (which was obtained in Example 10) according to the procedure of Example 179 as a pale yellowish solid; mp >140° C. (decomposed); 1H NMR (300 MHz, DMSO-d6) δ 1.25-1.40 (m, 2H), 1.75-1.95 (m, 2H), 2.50-3.60 (m, 7H), 2.88 (s, 3H), 3.16 (s, 2H), 4.47 (dd, J=8.0, 4.1 Hz, 1H), 6.78 (d, J=8.2 Hz, 1H), 6.84 (d, J=8.3 Hz, 2H), 6.95 (dd, J=8.2, 1.7 Hz, 1H), 7.05 (d, J=8.3 Hz, 2H), 7.16 (d, J=1.7 Hz, 1H); MS (ES) m/z: 464.1 (MH+); HRMS Calcd. for C22H28N3O6S(M−H)−: 462.1704. Found: 462.1696.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06525202B2
Source datasetuspto-grants-2003_02
ORD IDord-073459c203b94a30bd82a73b8c990504
Source noteuspto-grants-2003_02