Water → 2-(3-Bromo-2-hydroxymethyl-phenyl)-6-(1-hydroxy-1-methyl-ethyl)-3,4-dihydro-2H-isoquinolin-1-one

関与物質

役割	名称	HCID	仕込み量
反応物	Water	HCID 962	—
反応物	Sodium Bicarbonate	HCID 516892	—
反応物	Lithiumtriethylborohydride	HCID 23664628	—
反応物	2-Bromo-6-[6-(1-hydroxy-1-methyl-ethyl)-1-oxo-3,4-dihydro-1H-isoquinolin-2-yl]-benzaldehyde	HCID 86731002	—
溶媒	Tetrahydrofuran	HCID 8028	—
生成物	2-(3-Bromo-2-hydroxymethyl-phenyl)-6-(1-hydroxy-1-methyl-ethyl)-3,4-dihydro-2H-isoquinolin-1-one	HCID 71231050	—

反応手順

To a solution of Intermediate 42 (320 mg, 0.824 mmol) in THF (10 ml) under argon atmosphere was added lithium triethylborohydride (1M in THF, 0.989 ml, 0.989 mmol) dropwise. The resulting mixture was stirred for 2 hrs at r.t. before adding sat. aqueous NaHCO3 solution (5 ml). Additional water was added and the mixture was extracted three times with EtOAc. The combined organic layers were dried, filtered, and evaporated to dryness. The crude product was purified by flash chromatography (silica gel, cyclohexane/EtOAC gradient) to yield Intermediate 43.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09233111B2
出典データセット	uspto-grants-2016_01
ORD ID	ord-c2600f28670f415c8301abc3d3ada72d
出典メモ	uspto-grants-2016_01