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HRID 43942作成日:2026年10月25日

Cesium carbonate → Methyl cis(+/-)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-3-methylthiophene-2-carboxylate

https://huagongshe.com/reaction/43942

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 5-bromo-3-methylthiophene-2-carboxylateHCID 53438912—
反応物Benzyl cis(+/-)-[3-methoxypiperidin-4-yl]carbamateHCID 86648490—
触媒palladium(II) acetateHCID 167845—
生成物Methyl cis(+/-)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-3-methylthiophene-2-carboxylateHCID 8664882623.6%

反応手順

The same operation as in Example (244b) was performed using methyl 5-bromo-3-methylthiophene-2-carboxylate obtained in Example (245a) (218 mg, 0.93 mmol), benzyl cis(±)-(3-methoxypiperidin-4-yl)-carbamate obtained in Example (40b) (270 mg, 1.02 mmol), palladium acetate (42 mg, 0.19 mmol), BINAP (115 mg, 0.19 mmol) and cesium carbonate (423 mg, 1.30 mmol), to obtain 92 mg of the title compound as a yellow oily substance (24%).

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-9f771965f51343cb83a6d86cf4b28fbe
出典メモuspto-grants-2013_09