Dimethyl Sulfoxide → (2S,3S,4R,5R)-2-(3-Ethyl-[1,2,4]oxadiazol-5-yl)-5-(6-(1-ethyl-propylamino)-2-[2-(1-methyl-1H-imidazol-4-yl)-ethylamino]-purin-9-yl}tetrahydro-furan-3,4-diol formate

関与物質

役割	名称	HCID	仕込み量
反応物	Dimethyl Sulfoxide	HCID 679	—
反応物	1-Methylhistamine	HCID 3614	—
反応物	(2r,3r,4s,5s)-2-[2-Chloro-6-(1-ethyl-propylamino)-purin-9-yl]-5-(3-ethyl-[1,2,4]oxadiazol-5-yl)-tetrahydro-furan-3,4-diol	HCID 56625647	—
生成物	(2S,3S,4R,5R)-2-(3-Ethyl-[1,2,4]oxadiazol-5-yl)-5-(6-(1-ethyl-propylamino)-2-[2-(1-methyl-1H-imidazol-4-yl)-ethylamino]-purin-9-yl}tetrahydro-furan-3,4-diol formate	HCID 70020463	—

反応条件

温度	92.5 °C

反応手順

Intermediate 9 (0.070 g, 0.161 mmol) and 2-(1-methyl-1H-imidazol-4-yl)ethylamine (0.101 g, 0.807 mmol) were dissolved in DMSO (0.03 ml) and heated at 85-100° C. under nitrogen for 8 days, a further portion of 2-(1-methyl-1H-imidazol-4-yl)ethylamine (0.101 g, 0.807 mmol) was added after the first 5 days. The product was purified by Autoprep. HPLC to give the title compound after freeze drying as a cream solid (0.010 g). LC/MS system A Rt=3.36 min, m/z=526 MH+.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US06610665B1
出典データセット	uspto-grants-2003_08
ORD ID	ord-34d6f7ebeb87493e9b38bbb5999c2276
出典メモ	uspto-grants-2003_08