Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Potassium Carbonate → 1-(2-Chloro-3,6-difluorobenzyl)-8-methyl-7-[3-(morpholin-4-yl)phenyl]-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Potassium Carbonate | HCID 11430 | — |
| 반응물 | 4-(3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)morpholine | HCID 4192663 | — |
| 반응물 | 7-Bromo-1-(2-chloro-3,6-difluorobenzyl)-8-methyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine | HCID 67007063 | — |
| 촉매 | HCID 178418476 | HCID 178418476 | — |
| 용매 | N,N-Dimethylformamide--water (1/1) | HCID 21962138 | — |
| 생성물 | 1-(2-Chloro-3,6-difluorobenzyl)-8-methyl-7-[3-(morpholin-4-yl)phenyl]-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine | HCID 67008269 | 40% |
반응 단계
To a solution of 7-bromo-1-(2-chloro-3,6-difluorobenzyl)-8-methyl-1,2,3,4-tetrahydropyrido[2,3-b]pyrazine (0.048 g, 0.124 mmol) and 3-morpholinophenylboronic acid pinacol ester (0.035 g, 0.124 mmol) in DMF-H2O (9:1, 2 mL) was added PdCl2(PPh3)2 (0.0087 g, 0.0124 mmol) and K2CO3 (0.043 mg, 0.31 mmol). The resulting solution was subjected to microwave irradiation at 125° C. for 20 min. The solvent was filtered using a PTFE frit and then directly purified by prep HPLC using a gradient mixture of ACN—H2O— 0.1% TFA to yield the desired product (0.023 g 40%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US08846664B2 |
| 출처 데이터셋 | uspto-grants-2014_09 |
| ORD ID | ord-6e4ab137b7c647629183be7e639441a0 |
| 출처 메모 | uspto-grants-2014_09 |