4-Toluenesulfonyl chloride → HCID 178435363, compound

Participants

Reaction Steps

The title compound is prepared in a one pot reaction in analogy to Example 116 starting from 0.2 g (0.46 mmol) cis-{3-[4-amino-5-(3-benzyloxy-phenyl)-6-ethyl-pyrrolo[2,3-d]pyrimidin-7-yl]-cyclobutyl}-methanol of Example 124 and 0.18 g (0.92 mmol) p-toluenesulfonyl chloride in 2 ml dry pyridine followed by 2 ml pyrrolidine. The reaction is controlled by tlc. Analytical HPLC: tR=9.61 min (Grad 1); ES-MS: m/eo=482.0; NMR (DMSO-d6; not all signals reported): 8.12/s (1H); 6.9-7.5/several m's (6H), 7.05/“d” (1H); 6.95/s (1H); 6.92/“d” (1H); 5.4-6.0/b (NH2); 5.15/s (2H); 4.72/m (1H); 2.62/q (2H); 1.06/t (3H).

Provenance & Evidence