Formaldehyde → N-[(3,4-dichlorophenyl)methyl]-4-hydroxy-N-methyl-1-[2-(3-morpholinopropanoylamino)ethyl]-5-oxo-2H-pyrrole-3-carboxamide

関与物質

役割	名称	HCID	仕込み量
反応物	Formaldehyde	HCID 712	—
反応物	N-(2-amino-ethyl)-3-morpholin-4-yl-propionamide	HCID 21947517	—
反応物	3-[3-[3-[(3,4-dichlorophenyl)methyl-methyl-carbamoyl]-4-hydroxy-5-oxo-2H-pyrrol-1-yl]propanoylamino]propanoic acid	HCID 54691726	—
反応物	N-(3,4-Dichloro-benzyl)-2-(2,2-dimethyl-5-oxo-[1,3]dioxolan-4-ylidene)-N-methyl-acetamide	HCID 69655735	—
生成物	N-[(3,4-dichlorophenyl)methyl]-4-hydroxy-N-methyl-1-[2-(3-morpholinopropanoylamino)ethyl]-5-oxo-2H-pyrrole-3-carboxamide	HCID 54698208	—

反応手順

N-(3,4-Dichloro-benzyl)-2-(2,2-dimethyl-5-oxo-[1,3]dioxolan-4-ylidene)-N-methyl-acetamide (Compound 37-A) was treated with paraformaldehyde and N-(2-amino-ethyl)-3-morpholin-4-yl-propionamide as described in the preparation of Compound 37. The desired product was isolated as a white solid (0.0134 g, 5% yield). 1H NMR (300 MHz, CDCl3) δ: 2.41 (m, 2H), 2.64 (bs, 2H), 2.72 (bs, 2H), 2.98 (m, 2H), 3.03 (s, 3H), 3.51 (t, J=5.6 Hz, 2H), 3.63 (t, J=5.2 Hz, 2H), 3.78 (m, 4H), 4.35 (s, 2H), 4.59 (s, 2H), 7.11 (d, J=8.1 Hz, 1H), 7.35–7.44 (m, 3H), 8.27 (t, 1H). HRMS (M+H) calcd for C22H28N4Cl2O5: 497.13585. found: 497.1377.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07109186B2
出典データセット	uspto-grants-2006_09
ORD ID	ord-b4c4d6cde14149838ceb9363e1ac4cef
出典メモ	uspto-grants-2006_09