(S)-5-(Hydroxymethyl)-2-pyrrolidinone → [(2S)-5-oxotetrahydro-1H-2-pyrrolyl]methyl N-[4-(4-amino-7-tetrahydro-2H-4-pyranyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methoxyphenyl]carbamate

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Reaktionsschritte

Phenyl N-[4-(4-amino-7-tetrahydro-2H-4-pyranyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methoxyphenyl]carbamate (30 mg, 0.065 mmol) was mixed with (5S)-5-(hydroxymethyl)tetrahydro-1H-2-pyrrolone (0.05 mL) in pyridine (0.5 mL). The reaction mixture was heated at 100° C. overnight. The solvent was removed and the residue was purified by preparative reverse phase LC/MS to give [(2S)-5-oxotetrahydro-1H-2-pyrrolyl]methyl N-[4-(4-amino-7-tetrahydro-2H-4-pyranyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methoxyphenyl]carbamate (10 mg, 0.02lmmol). 1H NMR (CDCl-d) δ 1.90(m, 1H), 2.06(m, 4H), 2.34(m, 1H), 2.41(m, 2H), 3.64(m, 2H), 3.94 (s, 3H), 4.04(m, 2H), 4.14(m, 2H), 4.98(m, 1H), 5.33(m, 3H), 6.10(s, 1H), 6.98(s, 1H), 7.04 (s, 1H), 7.09(m, 1H), 7.31(s, 1H), 8.11(bs, 1H), 8.32(s, 1H). LC/MS: MH+481.

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