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HRID 79304作成日:2026年10月25日

Cesium carbonate → (S)-tert-butyl 3-(6-((3-ethyl-4-(imidazo[1,2-a]pyridine-3-carboxamido)-1H-indazol-1-yl)methyl)pyridin-2-yloxy)pyrrolidine-1-carboxylate

https://huagongshe.com/reaction/79304

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Tert-butyl (3R)-3-(methanesulfonyloxy)pyrrolidine-1-carboxylateHCID 10934372—
反応物HCID 178437935HCID 178437935—
溶媒DimethylacetamideHCID 31374—
生成物(S)-tert-butyl 3-(6-((3-ethyl-4-(imidazo[1,2-a]pyridine-3-carboxamido)-1H-indazol-1-yl)methyl)pyridin-2-yloxy)pyrrolidine-1-carboxylateHCID 7081488050.6%

反応条件

温度90 °C

反応手順

To N-(3-ethyl-1-((6-hydroxypyridin-2-yl)methyl)-1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide (21 mg, 0.051 mmol) in DMA (2 mL) was added (R)-tert-butyl 3-(methylsulfonyloxy)pyrrolidine-1-carboxylate (20 mg, 0.076 mmol) and Cs2CO3 (33 mg, 0.10 mmol). The reaction vial was sealed, and the reaction was heated to 90° C. and stirred for 6 hours. DMA was removed under reduce pressure. The residue was diluted with EtOAc (20 mL), washed with saturated NaHCO3 aqueous solution (5 mL) and brine (5 mL), and concentrated. Silica gel chromatography of the crude material (DCM/MeOH 10:0.5) provided the desired product (15 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08841455B2
出典データセットuspto-grants-2014_09
ORD IDord-1885a0e738a94714aea0ffd29319f71a
出典メモuspto-grants-2014_09