Reaktion #68808

Reaktionsgleichung

3-(4-cyclopropylmethoxy-phenoxy)-azetidine

N-[1-(4-bromo-phenyl)-1-methyl-ethyl]-acetamide

NaOtBu

2-(di-tert-butylphosphino)biphenyl

→

desired product

N-(1-{4-[3-(4-Cyclopropylmethoxy-phenoxy)-azetidin-1-yl]-phenyl}-1-methyl-ethyl)-acetamide

Lösungsmittel

THF

Reaktionsbedingungen

Aufarbeitung

1. 1
   FiltrationThe mixture is filtered
2. 2
   Einengenconcentrated in vacuo
3. 3
   SonstigeThe residue is purified by HPLC (Zorbax, acetronitrile/H2O (+0.15% HCOOH))

Vorschrift

To 35 mg (0.16 mmol) 3-(4-cyclopropylmethoxy-phenoxy)-azetidine (IX.1) in THF (2.0 mL) are added under an argon atmosphere 41 mg (0.16 mmol) N-[1-(4-bromo-phenyl)-1-methyl-ethyl]-acetamide, 63 mg (0.64 mmol) NaOtBu, 19 mg (0.064 mmol) 2-(di-tert-butylphosphino)biphenyl and 15 mg (0.016 mmol) tris-(dibenzylidene-acetone)-dipalladium(0). The mixture is stirred for 12 h at 45° C. The mixture is filtered and concentrated in vacuo. The residue is purified by HPLC (Zorbax, acetronitrile/H2O (+0.15% HCOOH)) to yield the desired product.

Quelle