Dimethylformamide → HCID 178472577、化合物

関与物質

役割	名称	HCID	仕込み量
反応物	Dimethylformamide	HCID 6228	—
反応物	Diisopropylethylamine	HCID 81531	—
反応物	Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)	HCID 9886157	—
反応物	(2R,4R)-4-amino-5-(3'-chlorobiphenyl-4-yl)-2-hydroxypentanoic acid ethyl ester	HCID 86682253	—
反応物	HCID 178481916	HCID 178481916	—
生成物	HCID 178472577	HCID 178472577	27.3%

反応手順

5-Hydroxy-1-methyl-1h-pyrazole-3-carboxylic acid (122 mg, 862 μmol) and HATU (361 mg, 949 μmol) were combined in DMF (1.0 mL, 13 mmol) and stirred for 10 minutes. (2R,4R)-4-amino-5-(3′-chlorobiphenyl-4-yl)-2-hydroxypentanoic acid ethyl ester (30.0 mg, 86 μmol) and DIPEA (165 μL, 949 μmol) were added, and the resulting mixture was stirred at room temperature overnight. The mixture was then concentrated under reduced pressure and the residue was dissolved in 50% AcOH-water (1.5 mL), filtered, purified by reverse phase preparative HPLC, and lyophilized to yield the title compound (11.1 mg). MS m/z [M+H]+ calc'd for C24H26ClN3O5, 472.16. found 472.2.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09108934B2
出典データセット	uspto-grants-2015_08
ORD ID	ord-a1e22c1b7ca94f548df0a5cbf19ac39c
出典メモ	uspto-grants-2015_08