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HRID 1663032作成日:2026年10月25日

Isoquinoline, 1-chloro- → [1-(1-Isoquinolyl)-4-piperidyl]methanol

https://huagongshe.com/reaction/1663032

反応式

関与物質

役割名称HCID仕込み量
反応物Isoquinoline, 1-chloro-HCID 140539—
反応物4-PiperidinemethanolHCID 420771—
反応物Binap, (A+-)-HCID 634876—
反応物Sodium t-butoxideHCID 23676156—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
生成物[1-(1-Isoquinolyl)-4-piperidyl]methanolHCID 21096912—

反応手順

The process is performed as described in Example 2 (step 2.1). Starting with 2.50 g (15.28 mmol) of 1-chloroisoquinoline, 1.94 g (136.6 mmol) of 4-piperidylmethanol, 3.53 g (36.67 mmol) of sodium tert-butoxide, 0.285 g (0.46 mmol) of BINAP and 0.140 g (0.15 mmol) of tris(dibenzylideneacetone)dipalladium, and after chromatography on silica gel, eluting with a 98/2/0.2 and then 95/5/0.5 mixture of dichloromethane, methanol and 28% aqueous ammonia, 2.40 g of pure product are obtained in the form of a viscous orange oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08034818B2
出典データセットuspto-grants-2011_10
ORD IDord-922d58f6a38145bca556ab8248623dfd
出典メモuspto-grants-2011_10