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HRID 1432975作成日:2026年10月26日

2-[(5-Chlorothiophen-2-yl)oxy]acetic acid → 1-(4-Amino-quinazolin-7-ylmethyl)-4-[(5-chloro-thiophen-2-yloxy)-acetyl]-3-(S)-propyl-piperazin-2-one

https://huagongshe.com/reaction/1432975

反応式

関与物質

役割名称HCID仕込み量
反応物2-[(5-Chlorothiophen-2-yl)oxy]acetic acidHCID 11183144—
反応物1-(4-Aminoquinazoline-7-ylmethyl)-3-propyl-piperazine-2-oneHCID 17985268—
生成物1-(4-Amino-quinazolin-7-ylmethyl)-4-[(5-chloro-thiophen-2-yloxy)-acetyl]-3-(S)-propyl-piperazin-2-oneHCID 9956530—

反応手順

The title compound is prepared as described in EXAMPLE 123, using 1-(4-aminoquinazoline-7-ylmethyl)-3-propyl-piperazine-2-one, EXAMPLE 78 and 5-chloro-2-thienyloxyacetic acid, EXAMPLE 24. 1H NMR (d6-DMSO, 300 MHz) δ9.78 (bs, 2H), 8.81 (s, 1H), 8.35 (d, 1H), 7.60 (m, 2H), 7.51 (s, 1H), 6.69 (m, 1H), 6.21 (d, 1H), 4.91 (AB, 2H), 4.72 (m, 2H), 3.84 (m, 1H), 3.52 (m, 2H), 3.23 (m, 1H), 1.80 (m, 2H), 1.24 (m, 2H), 0.82 (m, 3H). MS (ion spray), m/z, 474, 476, (M+H) (Cl pattern). Elemental analysis, cal C22H22ClN5O2S.C2HF3O2.1.15H2O % C=47.31, % H=4.52, % N=11.50; found % C=47.39, % H=4.140, % N=11.19.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07612075B2
出典データセットuspto-grants-2009_11
ORD IDord-f0c8b4fbe35546b48878659b93b0e1c1
出典メモuspto-grants-2009_11