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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 245911생성일: 2026년 10월 26일

Water → 2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanylethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid ((R)-2,2-difluoro-1-methyl-propyl)-amide

https://huagongshe.com/reaction/245911

반응식

참여 물질

역할이름HCID투입량
반응물WaterHCID 962—
반응물DiisopropylethylamineHCID 81531—
반응물Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 9886157—
반응물2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acidHCID 71279620—
반응물(R)-2,2-difluoro-1-methyl-propylamine trifluoroacetateHCID 86677918—
용매DimethylformamideHCID 6228—
생성물2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanylethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid ((R)-2,2-difluoro-1-methyl-propyl)-amideHCID 7128608081%

반응 단계

In a round-bottomed flask, (R)-2,2-difluoro-1-methyl-propylamine trifluoroacetate (crude from Step 4) was dissolved in DMF (1.2 ml) and N,N-diisopropylethylamine (0.5 ml, 2.86 mmol) was added. Then 2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid (110 mg, 0.25 mmol) was added followed by HATU (104 mg, 0.27 mmol). The yellow solution was stirred at room temperature overnight. Water was added and the suspension was filtered. The filter cake was washed with water and petroleum ether then dried under high vacuum to afford 108 mg (81%) of 2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid ((R)-2,2-difluoro-1-methyl-propyl)-amide as an off-white powder.

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US08658646B2
출처 데이터셋uspto-grants-2014_02
ORD IDord-0132097983cb4364a87047221a3419ad
출처 메모uspto-grants-2014_02