1-Hydroxybenzotriazole → 2-(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)-N-[4-(4-isobutylphenyl)-1,3-thiazol-2-yl]acetamide

참여 물질

역할	이름	HCID	투입량
반응물	1-Hydroxybenzotriazole	HCID 75771	—
반응물	4-(4-Isobutylphenyl)-1,3-thiazol-2-amine	HCID 869862	—
반응물	1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride	HCID 2723939	—
반응물	1,3,5-trimethylthieno[3,4-d]pyrimidine-2,4(1H,3H)-dione	HCID 71008093	—
촉매	4-(Dimethylamino)pyridine	HCID 14284	—
용매	1,2-Dichloroethane	HCID 11	—
생성물	2-(1,3-Dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)-N-[4-(4-isobutylphenyl)-1,3-thiazol-2-yl]acetamide	HCID 46927772	—

반응 단계

The title compound was prepared according to the general procedure (Method A) by coupling Intermediate 1 (100 mg, 0.393 mmol) with 4-(4-isobutylphenyl)-1,3-thiazol-2-amine (91 mg, 0.393 mmol) in the presence of EDCI hydrochloride (90 mg, 0.472 mmol), HOBt (16 mg, 0.117 mmol) and DMAP (5 mg, 0.039 mmol) in 1,2 dichloroethane (4 ml) to give 42 mg of the product as a white solid; 1H NMR (300 MHz, CDCl3) δ 0.88 (d, J=6.3 Hz, 6H), 1.83-1.90 (m, 1H), 2.48 (d, J=6.9 Hz, 2H), 3.51 (s, 3H), 3.57 (s, 3H), 4.06 (s, 2H), 6.88 (s, 1H), 7.04 (s, 1H), 7.16 (d, J=7.8 Hz, 2H), 7.72 (d, J=7.8 Hz, 2H), 10.73 (br s, 1H); APCI-MS (m/z) 469.14 (M+H)+.

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08987278B2
출처 데이터셋	uspto-grants-2015_03
ORD ID	ord-ac3f929e76f54bce85f160a3c00cc5e2
출처 메모	uspto-grants-2015_03