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HRID 1754833作成日:2026年10月24日

Triethylamine → (+/-)-{4-Chloro-2-[5-(2-methoxy-benzylthiocarbamoyl)-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-4-yl]-phenoxy}-acetic acid

https://huagongshe.com/ja/reaction/1754833

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Sodium HydroxideHCID 14798—
反応物2-Methoxybenzyl isothiocyanateHCID 140256—
反応物(+/-)-[4-Chloro-2-(4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-4-yl)-phenoxy]-acetic acid ethyl ester hydrochlorideHCID 90021828—
溶媒Formic AcidHCID 284—
溶媒AcetonitrileHCID 6342—
生成物(+/-)-{4-Chloro-2-[5-(2-methoxy-benzylthiocarbamoyl)-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-4-yl]-phenoxy}-acetic acidHCID 72948702—

反応手順

To a solution of (±)-[4-chloro-2-(4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-4-yl)-phenoxy]-acetic acid ethyl ester hydrochloride (50 mg, 0.13 mmol, 1.00 eq.) and NEt3 (54 μL, 0.39 mmol, 3.00 eq.) in MeCN (1 mL), 2-methoxybenzyl isothiocyanate (24 mg, 0.14 mmol, 1.05 eq.) in MeCN (1 mL) was added. The mixture was stirred at r.t. for 18 hours. 1M aq. NaOH (0.5 mL) was added. The mixture was stirred at r.t. for 18 hours. The solution was neutralized with formic acid, purified by prep. HPLC (column: Atlantis, 30×75 mm, 10 um, UV/MS, acidic conditions), and concentrated in vacuo to give the desired acid as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09169270B2
出典データセットuspto-grants-2015_10
ORD IDord-c0b01d7c0be74736aacdc50b232042f4
出典メモuspto-grants-2015_10