Phthalimide → HCID 178508597, compound

Participants

Reaction Steps

To a solution of 3.5 g (8.74 mmol) of cis-{3-[4-amino-5-(3-benzyloxy-phenyl)-pyrrolo[2,3-d]pyrimidin-7-yl]-cyclobutyl)methanol, which is prepared as described in Example 47(b) of WO 97/28161, in 70 ml of dry THF are added under argon 2.75 g (10.5 mmol) of triphenylphosphine and 1.54 g (10.5 mmol) of phthalimide; 1.9 g (1.71 ml; 10.5 mmol) of diethyl azodicarboxylate (96%) are added dropwise thereto. After stirring for 16 h at RT, the solution is concentrated to dryness and the crude compound is purified by flash-chromatography (ethylacetate) to provide cis-2-{3-[4-amino-5-(3-benzyloxy-phenyl)-pyrrolo[2,3-d]pyrimidin-7-yl]-cyclobutylmethyl}isoindole-1,3-dione. Analytical HPLC: tR=11.96 min (Grad 1); ES-MS: m/eo=529.9.

Provenance & Evidence