Triethylamine → HCID 25095901, compound

Participants

Reaction Conditions

Reaction Steps

Dissolve 200 mg (0.5 mmol) of (+/−)-5-(4-methoxyphenyl)-6-phenyl-4-(piperidin-3-yloxy)furo-[2,3-d]pyrimidine (Example 37A) in 1 ml of THF and add 69 μl (0.5 mmol) of triethylamine. After adding 54 μl (0.5 mmol) of 3-bromopropionic acid methyl ester, stir the mixture at 20-40° C. for approx. 8 h. In the meantime, add triethylamine (total of approx. 1.2 mmol) and 3-bromopropionic acid methyl ester (total of approx. 1.2 mmol) twice more. After diluting with dichloromethane, wash the mixture with saturated sodium hydrogencarbonate solution and concentrate under reduced pressure. Purify the crude product by means of preparative RP-HPLC (eluent: acetonitrile/water gradient). 118 mg (45.7% of theory) of the target product are obtained.

Provenance & Evidence