Reaction Steps
A solution of (1R,2R)-3-[2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]-6-[4-imino(methoxy)methyl]phenyl]thieno[3,2-d]pyrimidin-4(3H)-one (0.35 g, 0.652 mmol) (obtained in example 63) and 1N HCl (2 mL) in MeOH (15 mL) was allowed to react at room temperature overnight. The solvent was removed by concentration and the residue was partitioned between CHCl3 and 10% NaHCO3 solution. The organic phase was separated, dried over Na2SO4, filtered, concentrated and purified by flash chromatography to give the title compound as a white solid: mp 280°-285° C.; 1H NMR (300 MHz, CDCl3) δ (TMS) 8.61 (s, 1H, N=CH--N), 7.92 (d, Jt =8.4, 2H, arom), 7.81 (d, Jt =8.4, 2H, arom), 7.78 (s, 1H, triazole), 7.74 (s, 1H, triazole, 7.63 (s, 1H, thiophene), 7.49 (dt, Jd =6.4, Jt =8.8, 1H, arom), 6.9-6.7 (m, 2H, arom), 6.2-5.5 (broad signal, 2H, NH2), 5.98 (dq, Jd =1.6, Jq =7.3, 1H, MeCH), 5.56 (d, J=1.6, 1H, OH), 5.20 (d, J=14.2, 1H, CH(H)), 4.03 (d, J=14.2, 1H, CH(H)), 1.32 (d, J=7.3, 3H, CHMe); MS 299 (N-ethylheterocycle, C15H13N3O2 S), 224 (Tr--CH2COHAr, C10H8F2N3O); [α]D =+63.6° (c 1, MeOH).
