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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1641977Generated: November 2, 2026

4-(2-Aminoethyl)benzoic acid → 4-{2-[3-((R)-1-{6-(2,2-Diphenyl-ethylamino)-9-[(1R,2S,3R,4S)-4-(5-ethyl-tetrazol-2-yl)-2,3-dihydroxy-cyclopentyl]-9H-purin-2-yl}-pyrrolidin-3-yl)-ureido]-ethyl}-benzoic acid hydrochloride

https://huagongshe.com/reaction/1641977

Reaction equation

Participants

RoleNameHCIDCharge
Reactant4-(2-Aminoethyl)benzoic acidHCID 506066—
Reactant(1R,2S,3R,5S)-3-[2-((R)-3-amino-pyrrolidin-1-yl)-6-(2,2-diphenyl-ethylamino)-purin-9-yl]-5-(5-ethyl-tetrazol-2-yl)-cyclopentane-1,2-diolHCID 11650095—
Reactant1-((R)-1-{6-(2,2-Diphenyl-ethylamino)-9-[(1R,2S,3R,4S)-4-(5-ethyl-tetrazol-2-yl)-2,3-dihydroxy-cyclopentyl]-9H-purin-2-yl}-pyrrolidin-3-yl)-3-pyridin-2-ylmethyl-urea hydrochlorideHCID 66735772—
Product4-{2-[3-((R)-1-{6-(2,2-Diphenyl-ethylamino)-9-[(1R,2S,3R,4S)-4-(5-ethyl-tetrazol-2-yl)-2,3-dihydroxy-cyclopentyl]-9H-purin-2-yl}-pyrrolidin-3-yl)-ureido]-ethyl}-benzoic acid hydrochlorideHCID 66736716—

Reaction Steps

This compound is prepared from ((1R,2S,3R,5S)-3-[2-((R)-3-amino-pyrrolidin-1-yl)-6-(2,2-diphenyl-ethylamino)-purin-9-yl]-5-(5-ethyl-tetrazol-2-yl)-cyclopentane-1,2-diol (Example 48) using a procedure analogous to that of 1-((R)-1-{6-(2,2-diphenyl-ethylamino)-9-[(1R,2S,3R,4S)-4-(5-ethyl-tetrazol-2-yl)-2,3-dihydroxy-cyclopentyl]-9H-purin-2-yl}-pyrrolidin-3-yl)-3-pyridin-2-ylmethyl-urea hydrochloride (Example 113) by replacing 2-aminomethyl pyridine with 4-(2-amino-ethyl)-benzoic acid. MS (ES+) m/e 787.51 (MH+)

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08114877B2
Source datasetuspto-grants-2012_02
ORD IDord-eb871e607c7f48d3909647c8152fcad6
Source noteuspto-grants-2012_02