Pyridine → HCID 178421986, compound

Participants

Reaction Steps

The title compound is prepared in analogy to Example 116 starting from 0.35 g (0.84 mmol) cis-{3-[4-amino-5-(3-benzyloxy-phenyl)-6-methyl-pyrrolo[2,3-d]pyrimidin-7-yl]-cyclobutyl}-methanol and 0.328 g (1.69 mmol) p-toluenesulfonyl chloride in 3.5 ml dry pyridine, followed by 0.442 ml (6.33 mmol) trimethylenimine (Fluka, Buchs, Switzerland). Analytical HPLC: tR=9.22 min (Grad 1); ES-MS: m/eo=454.3; NMR (DMSO-d6): 8.08/s (1H), 7.25-7.5/several m's (6H), 7.02/“d” (1H); 6.93/s (1H); 6.89/“d” (1H); 5.4-6.0/b (NH2); 5.13/s (2H); 4.76/m (1H); 3.11/“t” (4H); 2.75-2.90/m (2H); 2.54/d (2H); 2.35-2.45/m (2H); 2.22/s (3H); 2.03/m (1H); 1.9-2.0/m (2H).

Provenance & Evidence