4-Bromocrotonic acid → 8-{(2E)-4-[Cyclopropyl(methyl)amino]but-2-enoyl}-N-(3,4-dichlorophenyl)-6,7,8,9-tetrahydro-5H-pyrimido[5',4':4,5]thieno[2,3-c]azepin-4-amine

Participants

Reaction Steps

In analogy to Example 130, the title compound was prepared from (2E)-4-bromobut-2-enoic acid (127 mg, 0.62 mmol), N-(3,4-dichlorophenyl)-6,7,8,9-tetrahydro-5H-pyrimido[5′,4′:4,5]thieno[2,3-c]azepin-4-amine from Example 82A (150 mg, 0.41 mmol) and N-methylcyclopropanamine (116 mg, 1.63 mmol) to yield 21 mg (10%).

Provenance & Evidence