Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
Pyrimidine-5-carboxylic acid → Pyrimidine-5-carboxylic acid {4-[3-cyclopropylmethyl-1-(2-fluorobenzyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-ylmethyl]-phenyl}-methyl-amide
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|---|---|---|
| 반응물 | Pyrimidine-5-carboxylic acid | HCID 78346 | — |
| 반응물 | 3-Cyclopropylmethyl-8-[4-(methylamino)-benzyl]-1-(2-fluorobenzyl)-3,7-dihydropurine-2,6-dione | HCID 21891691 | — |
| 촉매 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 생성물 | Pyrimidine-5-carboxylic acid {4-[3-cyclopropylmethyl-1-(2-fluorobenzyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-ylmethyl]-phenyl}-methyl-amide | HCID 10098770 | 72% |
반응 단계
This compound was prepared by a method similar to that described in example 79 except that pyrimidine-5-carboxylic acid was used in place of N-acetyl-6-amino-2-pyridine carboxylic acid, the reaction was performed using 0.75 equivalents of 3-cyclopropylmethyl-8-[4-(methylamino)-benzyl]-1-(2-fluorobenzyl)-3,7-dihydropurine-2,6-dione and 1.5 equivalent of 4-dimethylaminopyridine was added as the final reagent to the reaction mixture. Purification was performed by chromatography using silica eluted with 94:6 ethyl acetate/methanol followed by trituration with hot acetonitrile to give the product as a colorless solid (72%). MS, m/z(M+H)=540.2161.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 특허 번호 | US07135475B2 |
| 출처 데이터셋 | uspto-grants-2006_11 |
| ORD ID | ord-960f7c3a7ff645c88818ed6d406b2f06 |
| 출처 메모 | uspto-grants-2006_11 |