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【结 构 式】 
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【分子编号】40653 【品名】1-(2-methyl-5-pyrimidinyl)-1,2-dihydrophthalazine 【CA登记号】 |
【 分 子 式 】C13H12N4 【 分 子 量 】224.26524 【元素组成】C 69.62% H 5.39% N 24.98% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(XII)Lithiopyrimidine (X), prepared from 5-bromo-2-methylpyrimidine (IX) was added to phthalazine (XI) to produce adduct (XII). Displacement of ester (VIII) by dihydrophthalazine (XII) in the presence of butyllithium furnished the corresponding racemic amide. The desired (R)-enantiomer was finally isolated by chiral chromatography on a Chiralpak AD column.
| 【1】 Guerry, P.; Locher, H.H.; Hubschwerlen, C.; Wyss, P.C.; Jolidon, S.; Hartman, P.G.; Stalder, H.; Specklin, J.L.; Anti-MRSA dihydrofolate reductase inhibitors: Synthesis and SAR. 39th Intersci Conf Antimicrob Agents Chemother (Sept 26 1999, San Francisco) 1999, Abst F1800. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (IX) | 40650 | 5-bromo-2-methylpyrimidine | C5H5BrN2 | 详情 | 详情 | |
| (X) | 40651 | (2-methyl-5-pyrimidinyl)lithium | C5H5LiN2 | 详情 | 详情 | |
| (XI) | 40652 | phthalazine | 253-52-1 | C8H6N2 | 详情 | 详情 |
| (XII) | 40653 | 1-(2-methyl-5-pyrimidinyl)-1,2-dihydrophthalazine | C13H12N4 | 详情 | 详情 | |
| (XIII) | 40649 | ethyl (E)-3-[5-[(2,4-diamino-5-pyrimidinyl)methyl]-2,3-dimethoxyphenyl]-2-propenoate | C18H22N4O4 | 详情 | 详情 |
Extended Information