1-Hydroxybenzotriazole → (2R)-4-{4-[2-(2-Aminopyrimidin-5-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-8-yl]piperazin-1-yl}-4-oxobutan-2-ol

참여 물질

역할	이름	HCID	투입량
반응물	1-Hydroxybenzotriazole	HCID 75771	—
반응물	3-Hydroxybutanoic acid, (R)-	HCID 92135	—
반응물	1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride	HCID 2723939	—
반응물	5-(9-Isobutyl-6-morpholino-8-(piperazin-1-yl)-9H-purin-2-yl)pyrimidin-2-amine	HCID 59333501	—
용매	Dimethylformamide	HCID 6228	—
생성물	(2R)-4-{4-[2-(2-Aminopyrimidin-5-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-8-yl]piperazin-1-yl}-4-oxobutan-2-ol	HCID 45376241	36%

반응 단계

5-(9-Isobutyl-6-morpholin-4-yl-8-piperazin-1-yl-9H-purin-2-yl)pyrimidin-2-amine (150 mg, 0.33 mmol), 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride (128 mg, 0.67 mmol), 1-hydroxybenzotriazole (45 mg, 0.33 mmol), and (R)-3-hydroxybutyric acid (70 mg, 0.67 mmol) were dissolved in dimethylformamide (5 ml) and the resulting mixture was stirred for 16 hours. The solvent was evaporated under reduced pressure and then the residue was purified by preparative HPLC (column, NOMURA Develosil Combi-RP-5; mobile phase, acetonitrile/water/formic acid) to give the title compound (62 mg, 36%) as a white solid.

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08097622B2
출처 데이터셋	uspto-grants-2012_01
ORD ID	ord-3113a6c2724a4320a14277ab2e4b73c1
출처 메모	uspto-grants-2012_01