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

関与物質

役割	名称	HCID	仕込み量
反応物	4-Bromocrotonic acid	HCID 6436411	—
反応物	N-Methylcyclopropanamine	HCID 11029756	—
反応物	N-(3,4-Dichlorophenyl)-6,7,8,9-tetrahydro-5H-pyrimido[5',4':4,5]thieno[2,3-c]azepin-4-amine	HCID 58116941	—
生成物	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	HCID 25220993	—

反応手順

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%).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08524722B2
出典データセット	uspto-grants-2013_09
ORD ID	ord-8f5fca2e8f3b44728c6d2cc1c9ec8754
出典メモ	uspto-grants-2013_09