Reaktion #63238

ord-ac4c27ac2f6f4849b7ba4003c0c8aa14

Reaktionsbedingungen

Temperatur
25°CELSIUS
Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    workup.STIRRINGstirred at 25° C. for 18 hours

Vorschrift

A solution of 3.0 g (35.3 mmol) of anhydrous 5-aminotetrazole in 20 ml of dimethyl sulfoxide is added dropwise to a 15° to 20° C. slurry of 2.8 g (70.0 mmol) of 60% NaH (oil dispersion) in 75 ml of dimethyl sulfoxide under nitrogen atmosphere. The resulting mixture is stirred at 25° C. for 2.5 hours. A solution of 6.50 g (28.98 mmol) of methyl 4-methoxy-2-(1-methylethoxy)benzoate in 25 ml of dimethyl sulfoxide is added dropwise to the reaction and stirred at 25° C. for 18 hours. The reaction is poured onto 600 g of ice-water and the resulting aqueous solution is acidified with aqueous 10% HCl. The product is isolated by vacuum filtration and recrystallization from 95% ethanol gives 1.90 g (8.03 g theoretical, 24%) of the analytically pure 4-methoxy-2-(1-methylethoxy)-N-1H-tetrazol-5-ylbenzamide as fine, white needles having a melting point of 212° -213° C.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US04764525uspto-grants-1988_08