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HRID 588156作成日:2026年10月26日

Methylcarbamoyl chloride → (6-chloro-3-methoxy-1-trityl-1H-pyrazolo[4,3-c]pyridin-4-yl)methyl methylcarbamate

https://huagongshe.com/reaction/588156

反応式

関与物質

役割名称HCID仕込み量
反応物Methylcarbamoyl chlorideHCID 80931—
反応物DiisopropylethylamineHCID 81531—
反応物(6-chloro-3-methoxy-1-trityl-1H-pyrazolo[4,3-c]pyridin-4-yl)methanolHCID 118271763—
溶媒DichloromethaneHCID 6344—
生成物(6-chloro-3-methoxy-1-trityl-1H-pyrazolo[4,3-c]pyridin-4-yl)methyl methylcarbamateHCID 11827230476.3%

反応条件

温度35 °C

反応手順

A solution of (6-chloro-3-methoxy-1-trityl-1H-pyrazolo[4,3-c]pyridin-4-yl)methanol (Intermediate 35B, 200 mg, 0.439 mmol) and methylaminoformyl chloride (45.1 mg, 0.483 mmol) in DCM (1462 μl) was treated with DIEA (153 μl, 0.877 mmol) and stirred @ 35° C. for 1 h Reaction was dilluted in with DCM and concentrated in vacuo on silica. Material was purified by normal phase column chromotography eluting with Hex/EtOAc (0-40%) affording (6-chloro-3-methoxy-1-trityl-1H-pyrazolo[4,3-c]pyridin-4-yl)methyl methylcarbamate (172 mg, 0.335 mmol, 76% yield) as a white solid. MS: [M+H]+ m/z 513.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09226922B2
出典データセットuspto-grants-2016_01
ORD IDord-7e22731b8e114406993c3d8de19fee65
出典メモuspto-grants-2016_01