1-(5-Phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-4-amine → 1-(2-Fluoro-4-methoxyphenoxy)-3-(1-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-4-ylamino)propan-2-ol

Participants

Reaction Steps

Synthesis followed SP6 (3 h), using 300 μmol 2-((2-fluoro-4-methoxyphenoxy)methyl)oxirane and 1-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-4-amine to give O-methylated intermediate 1-(2-fluoro-4-methoxyphenoxy)-3-(1-(5-phenylthieno[2,3-d]pyrimidin-4-yl)piperidin-4-ylamino)propan-2-ol upon purification by prep. TLC (1 mm silica gel, PE/CH2Cl2/MeOH 4:6:1) with 40% yield. Product was obtained by O-demethylation according to SP12 (1 h) with 37% yield (LCMS: detected [M+1]=495.2).

Provenance & Evidence