4-Toluenesulfonyl chloride → HCID 178421989, 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 0.87 g (8.44 mmol) 4-hydroxypiperidine (Fluka, Buchs, Switzerland). Analytical HPLC: tR=8.76 min (Grad 1); ES-MS: m/eo=498.2; NMR (DMSO-d6; not all signals reported): 8.07/s (1H), 7.25-7.5/several m's (6H), 7.01/“d” (1H); 6.94/s (1H); 6.89/“d” (1H); 5.13/s (2H); 4.76/m (1H); 4.51/d (OH); 2.22/s (3H).

Provenance & Evidence