N,N-Diisopropylmethylamine → (R)-methyl 2-(4-chloro-2-(2,4-dimethoxybenzyl)-7-fluoro-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)-4-methylpentanoate

関与物質

役割	名称	HCID	仕込み量
反応物	N,N-Diisopropylmethylamine	HCID 547370	—
反応物	Leucine methyl ester hydrochloride	HCID 2723695	—
反応物	4,6-dichloro-2-[(2,4-dimethoxyphenyl)methyl]-7-fluoro-1H,2H,3H-pyrrolo[3,4-c]pyridin-3-one	HCID 58317575	—
溶媒	Acetonitrile	HCID 6342	—
生成物	(R)-methyl 2-(4-chloro-2-(2,4-dimethoxybenzyl)-7-fluoro-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)-4-methylpentanoate	HCID 58317585	—

反応条件

温度	100 °C

反応手順

A mixture of 4,6-dichloro-2-(2,4-dimethoxybenzyl)-7-fluoro-1H-pyrrolo[3,4-c]pyridin-3(2H)-one (3 g, 8.08 mmol), (S)-methyl 2-amino-4-methylpentanoate hydrochloride (2.94 g, 16.16 mmol), and N-isopropyl-N-methylpropan-2-amine (3.76 mL, 24.25 mmol) in ACN (50 mL) was stirred at 100° C. for 3 d. The solvent was removed and the resulting residue was used in the next step without further purification. [M+H] calc'd for C23H27ClFN3O5, 480; found, 480.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09108970B2
出典データセット	uspto-grants-2015_08
ORD ID	ord-f841ab9bc87148b4adf520ab514a5b35
出典メモ	uspto-grants-2015_08