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HRID 912341作成日:2026年10月25日

Thiophosgene → 4-(2-Amino-pyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carbothioic acid [4-(morpholine-4-carbonyl)-phenyl]-amide

https://huagongshe.com/reaction/912341

反応式

関与物質

役割名称HCID仕込み量
反応物ThiophosgeneHCID 10040—
反応物4-(Morpholine-4-carbonyl)anilineHCID 577815—
反応物Bis-(4-methoxybenzyl)-[5-(2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)-pyrimidin-2-yl]-amineHCID 45258862—
反応物4-(4-Ethyl-piperazin-1-yl)-2,6-difluoro-phenylamineHCID 59244379—
生成物4-(2-Amino-pyrimidin-5-yl)-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carbothioic acid [4-(morpholine-4-carbonyl)-phenyl]-amideHCID 59244491—

反応手順

Using bis-(4-methoxy-benzyl)-[5-(2-morpholin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)-pyrimidin-2-yl]-amine (80.9 mg) and (4-amino-phenyl)-morpholin-4-yl-methanone (37.1 mg) obtained in Step B in Example 1-D-104 instead of 4-(4-ethyl-piperazin-1-yl)-2,6-difluoro-phenylamine, and thiophosgene (22.9 μl) instead of triphosgene, in the same manner as Step D in Example 1-D-18, 4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidine-7-carbothioic acid [4-(morpholine-4-carbonyl)-phenyl]-amide was obtained as a crude product. Further, in the same manner as Step D in Example 1-D-18, the desired compound (D-251) was obtained as a colorless solid (40.1 mg, 68%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08022205B2
出典データセットuspto-grants-2011_09
ORD IDord-359f82cf720f40e28e9ad49d9d55e593
出典メモuspto-grants-2011_09