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【结 构 式】 
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【分子编号】27747 【品名】3-(2,4-dimethoxyphenyl)-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-ol 【CA登记号】 |
【 分 子 式 】C16H17N3O3 【 分 子 量 】299.3294 【元素组成】C 64.2% H 5.72% N 14.04% O 16.04% |
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：(III)Aminopyrazole (I) was cyclized to pyrazolopyrimidine (III) by means of ethyl acetoacetate (II) in refluxing dioxan. Chlorination of (II) with POCl3 produced the corresponding chloro derivative (IV). This was then heated with an excess of amine (V) in a sealed vessel at 100 C to afford the target compound, which was isolated as the hydrochloride salt.
| 【1】 Chen, C.; Webb, T.R.; McCarthy, J.R.; Moran, T.J.; Wilcoxen, K.M. (Janssen Pharmaceutica NV; Neurocrine Biosciences Inc.); Pyrazolopyrimidines as CRF receptor antagonists. EP 0880523; JP 2000503661; WO 9729109 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 27746 | 4-(2,4-dimethoxyphenyl)-3-methyl-1H-pyrazol-5-amine | C12H15N3O2 | 详情 | 详情 | |
| (II) | 11819 | ethyl acetoacetate; ethyl 3-oxobutanoate；Acetoacetic ester;Ethyl beta-ketobutyrate;ethyl 3-oxobutyrate | 141-97-9 | C6H10O3 | 详情 | 详情 |
| (III) | 27747 | 3-(2,4-dimethoxyphenyl)-2,5-dimethylpyrazolo[1,5-a]pyrimidin-7-ol | C16H17N3O3 | 详情 | 详情 | |
| (IV) | 27748 | 2-(7-chloro-2,5-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)-5-methoxyphenyl methyl ether | C16H16ClN3O2 | 详情 | 详情 | |
| (V) | 27749 | N-(2-methoxyethyl)-1-propanamine | 43175-57-1 | C6H15NO | 详情 | 详情 |
Extended Information