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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1667511Generated: October 30, 2026

1-Pyrrolidineethanamine → N-benzyl-5-ethoxymethyl-2-methyl-N'-(2-pyrrolidin-1-yl-ethyl)-benzene-1,3-diamine

https://huagongshe.com/reaction/1667511

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1-PyrrolidineethanamineHCID 1344—
Reactant1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine)HCID 636044—
ReactantSodium t-butoxideHCID 23676156—
ReactantBenzyl-(3-bromo-5-ethoxymethyl-2-methyl-phenyl)-amineHCID 67416493—
CatalystBis(dibenzylideneacetone)palladiumHCID 9811564—
Solvent1,4-DioxaneHCID 31275—
ProductN-benzyl-5-ethoxymethyl-2-methyl-N'-(2-pyrrolidin-1-yl-ethyl)-benzene-1,3-diamineHCID 6741649058,786.801%

Reaction Conditions

Temperature95 °C

Reaction Steps

A mixture of benzyl-(3-bromo-5-ethoxymethyl-2-methyl-phenyl)-amine (1.253 g, 3.749 mmol), xantphos (134 mg, 0.232 mmol), 1-(2-aminoethyl)pyrrolidine (0.71 mL, 5.639 mmol), Pd2(dba)3 (10 mg, 0.120 mmol), NaOtBu (658 mg, 6.847 mmol) and anhydrous dioxane (40 mL) was heated to 95° C. for 14 h. The reaction was cooled, filtered through celite, rinsed with EtOAc and concentrated. Chromatography (EtOAc/MeOH) afforded N-benzyl-5-ethoxymethyl-2-methyl-N′-(2-pyrrolidin-1-yl-ethyl)-benzene-1,3-diamine (810 g) as an orange liquid. m/z (M+1) 368.36.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08044041B2
Source datasetuspto-grants-2011_10
ORD IDord-016b1de1baf144018cd665299772ed79
Source noteuspto-grants-2011_10