Acetic Acid → Cis-(6-benzhydryl-tetrahydropyran-3-yl)-(3,4-difluoro-benzyl)-amine

関与物質

役割	名称	HCID	仕込み量
反応物	Acetic Acid	HCID 176	—
反応物	3,4-Difluorobenzaldehyde	HCID 588088	—
反応物	Sodium cyanoborohydride	HCID 5003444	—
反応物	Cis-(6-benzhydryl-tetrahydropyran-3-yl)-amine	HCID 11565229	—
溶媒	1,2-Dichloroethane	HCID 11	—
溶媒	Methanol	HCID 887	—
生成物	Cis-(6-benzhydryl-tetrahydropyran-3-yl)-(3,4-difluoro-benzyl)-amine	HCID 66631767	80.3%

反応手順

Trans-5-amino-2-diphenylmethyl-tetrahydropyran 15 (0.1 g, 0.38 mmol) was reacted with 3,4-difluorobenzaldehyde (0.055 g, 0.38 mmol) in the presence of glacial acetic acid (0.023 g, 0.38 mmol) in 1,2-dichloroethane (20 ml), and NaCNBH3 (0.03 g, 0.45 mmol) in methanol (5 ml) (Procedure D) to give compound 16j (0.12 g, 80%).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08841464B2
出典データセット	uspto-grants-2014_09
ORD ID	ord-e60d72141e284ba6b0f9256b7410a83c
出典メモ	uspto-grants-2014_09