Reaktion #1933952

ord-d646af6446424e1d8bb8d1728370f53e

Lösungsmittel

Reaktionsbedingungen

Temperatur
180°CELSIUS
Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Extraktionextracted with EtOAc (40 mL)
  2. 2
    Waschenwashed with brine
  3. 3
    Trocknendried over Na2SO4
  4. 4
    EinengenThe organic layers were concentrated
  5. 5
    Sonstigepurified by column chromatography

Vorschrift

A mixture of 3-((3-bromopyridin-2-yl)oxy)cyclobutanamine hydrochloride (242 mg, 1 mmol), 2-chloro-benzothiazole (169 mg, 1 mmol) and DIEA (286 mg, 2 mmol) in NMP (10 mL) was heated to 180° C. for 2 hours in microwave. The reaction mixture was added water, extracted with EtOAc (40 mL), washed with brine and dried over Na2SO4. The organic layers were concentrated and purified by column chromatography to give N-(3-((3-bromopyridin-2-yl)oxy)cyclobutyl)benzo[d]thiazol-2-amine (225 mg, 0.6 mmol, yield 60%). ESI-MS (M+1): 376 calc. for C16H14BrN3OS 375.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US08952037B2uspto-grants-2015_02