Tetrahydrofuran → N5-[(4-fluorophenyl)methyl]-4,5-pyrimidinediamine

Beteiligte Stoffe

Reaktionsschritte

To a stirred mixture of 30 parts of N-(4-amino-5-pyrimidinyl)-4-fluorobenzamide and 360 parts of tetrahydrofuran were added portionwise 9.86 parts of lithium tetrahydroaluminate under nitrogen atmosphere. The mixture was stirred for 6 hours. Another portion of 10 parts of lithium tetrahydroaluminate was added portionwise and stirring was continued for 2 hours at room temperature. The reaction mixture was decomposed with water. The layers were separated. The aqueous phase was extracted with tetrahydrofuran. The combined organic layers were dried, filtered and evaporated. The residue was crystallized from acetonitrile. The product was filtered off and dried, yielding 18 parts (63.5%) of N5 -[(4-fluorophenyl)methyl]-4,5-pyrimidinediamine (interm. 12).

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