Triethylamine → HCID 86653764, compound

Participants

Reaction Conditions

Reaction Steps

Add 82 μl (0.749 mmol) of 3-bromopropanoic acid methyl ester and 104 μl (0.749 mmol) of triethylamine to a solution of 150 mg (0.375 mmol) of (+/−)-5-(4-methoxyphenyl)-6-phenyl-N-piperidin-3-ylfuro[2,3-d]pyrimidin-4-amine (Example 39A) in 0.75 ml of THF, and stir at 20-40° C. overnight. Dilute the mixture with dichloromethane and wash with saturated sodium hydrogencarbonate solution. After concentration under reduced pressure, stir the residue with methanol, filter off the precipitated product with suction and dry under high vacuum. Isolate a second product batch from the filtrate after concentration by preparative RP-HPLC (eluent: acetonitrile/water gradient). A total of 124 mg (67.1% of theory) of the target product are obtained.

Provenance & Evidence