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HRID 609610作成日:2026年10月27日

Triethylamine → N-[(1-(3-Phenoxypropyl)-4-piperidinyl)methyl]3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide

https://huagongshe.com/reaction/609610

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Benzene, (3-bromopropoxy)-HCID 68522—
反応物N-(4-Piperidylmethyl) 3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamideHCID 9839803—
溶媒DimethylformamideHCID 6228—
溶媒AcetonitrileHCID 6342—
生成物N-[(1-(3-Phenoxypropyl)-4-piperidinyl)methyl]3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamideHCID 9868253—

反応手順

A stirred solution of N-(4-piperidinylmethyl) 3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide (E21) (250 mg, 0.80 mmole) and triethylamine (0.25 ml, 1.8 mmole) in a mixture of acetonitrile (15 ml) and N,N-dimethylformamide (10 ml) was treated with 3-phenoxypropyl bromide (0.13 ml, 0.88 mmole) and the solution heated under reflux for 48 h. The mixture was allowed to cool, then concentrated in vacuo and the residue dissolved in ethyl acetate (25 ml) and washed with water (20 ml). The organic solution was dried (MgSO4), concentrated in vacuo and the residue purified by flash chromatography on silica gel eluting with 0-20% methanol/ethyl acetate to afford the title compound as a pale pink solid after trituation with ether (44mg) mp 120-126° C.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US05998409
出典データセットuspto-grants-1999_12
ORD IDord-6f7ffc8c04fe43f9bfd3454885448099
出典メモuspto-grants-1999_12