2-(4-Aminophenyl)ethylamine → N-(3-{2-[2-(4-Amino-phenyl)-ethylamino]-pyrimidin-4-yl}-benzyl)-N-(3-amino-propyl)-methanesulfonamide

関与物質

役割	名称	HCID	仕込み量
反応物	2-(4-Aminophenyl)ethylamine	HCID 72895	—
反応物	(3-{[3-(2-Chloro-pyrimidin-4-yl)-benzyl]-methanesulfonyl-amino}-propyl)-carbamic acid tert-butyl ester	HCID 86603242	—
反応物	methanol-d4 CDCl3	HCID 88519945	—
生成物	N-(3-{2-[2-(4-Amino-phenyl)-ethylamino]-pyrimidin-4-yl}-benzyl)-N-(3-amino-propyl)-methanesulfonamide	HCID 58603635	—

反応手順

Intermediate 4 from above was coupled with 4-(2-Amino-ethyl)-phenylamine following procedure F and the resulting product deprotected following procedure G. LC-MS showed the product had the expected M+H+ of 455. CDCl3-CD3OD, shifts relative to the solvent peak at 7.24 ppm) δ 8.1 (m, 2H) 7.9 (d, 1H) 7.5 (d, 1H) 7.4 (m, 1H) 7.2 (m, 3H) 7.1 (d, 2H) 4.4 (s, 2H) 3.7 (m, 2H) 3.2 (m, 4H) 2.9 (m, 2H) 2.8 (s, 3H) 2.6 (m, 2H) 1.6 (m, 2H).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08268822B2
出典データセット	uspto-grants-2012_09
ORD ID	ord-a5e441826d064fcca37b4a5b2351fd82
出典メモ	uspto-grants-2012_09