4-Methylmorpholine → HCID 178502211, compound

Participants

Reaction Steps

Analogously to Example 5, 283 mg (1.49 mmol) of N-methoxycarbonyl-(D/L)-tert-leucine in 3.3 ml of THF and 329 ;d (2.99 mmol) of NMM are activated with 214 μl (1.64 mmol) of isobutyl chloroformate and then reacted with 388 mg (1.49 mmol) of 3-amino-4-(3-chloro-phenylamino)-1H-pyrazolo[3,4-d]pyrimidine (see Step 1.6) for 20 hours. Column chromatography (SiO2; toluene/ethyl acetate=1:1) yields rac.-4-(3-chloro-phenylamino)-3-([2-methoxycarbonylamino-3,3-dimethyl-butyryl]-amino)-1H-pyrazolo[3,4-d]-pyrimidine; HPLC: tRet(grad20-100/20)=12.1; FARMS: (M+H)+432.

Provenance & Evidence