L-Alaninol → N-((S)-1-hydroxypropan-2-yl)-2-(1-(5-methyl-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)ethyl)-1-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-4-carboxamide

関与物質

役割	名称	HCID	仕込み量
反応物	L-Alaninol	HCID 80307	—
反応物	phenyl 2-(1-(5-methyl-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)ethyl)-1-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-4-carboxylate	HCID 89875412	—
溶媒	Tetrahydrofuran	HCID 8028	—
生成物	N-((S)-1-hydroxypropan-2-yl)-2-(1-(5-methyl-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)ethyl)-1-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-4-carboxamide	HCID 89874554	52%

反応条件

温度	90 °C

反応手順

A mixture of phenyl 2-(1-(5-methyl-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)ethyl)-1-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-4-carboxylate (20 mg, 0.042 mmol, Intermediate-91, single enantiomer) and (S)-2-aminopropan-1-ol in THF (1.0 mL) is heated at 90° C. overnight. The reaction mixture is concentrated. The residue is purified by preparative LC-MS to give 9.9 mg (52% yield) of the title compound.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09187475B2
出典データセット	uspto-grants-2015_11
ORD ID	ord-7ceb700fbfbb4ff9b1fdcf5ff47e3e80
出典メモ	uspto-grants-2015_11