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HRID 43780作成日:2026年10月24日

Cesium carbonate → Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoate

https://huagongshe.com/ja/reaction/43780

反応式

関与物質

役割名称HCID仕込み量
反応物Cesium carbonateHCID 10796—
反応物Binap, (A+-)-HCID 634876—
反応物Methyl 3-chloro-5-fluorobenzoateHCID 21942504—
反応物Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamate hydrochlorideHCID 86648698—
触媒palladium(II) acetateHCID 167845—
生成物Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-5-fluorobenzoateHCID 8664872934.5%

反応手順

The same operation as in Example (42a) was performed using benzyl cis(±)-[3-methoxypiperidin-4-yl]carbamate hydrochloride obtained in Example (160a) (165 mg, 0.55 mmol), methyl 3-chloro-5-fluorobenzoate (103 mg, 0.55 mmol), palladium acetate (12.3 mg, 0.05 mmol), BINAP (68.3 mg, 0.11 mmol) and cesium carbonate (536 mg, 1.65 mmol), to obtain 79 mg of the title compound as a yellow oily substance (35%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08536197B2
出典データセットuspto-grants-2013_09
ORD IDord-25c3092eb6694f7fb6faac504b527022
出典メモuspto-grants-2013_09