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发明公开
CN102372674A 医药中间体3-醛基-4-卤代吡唑的合成方法 无效 - 驳回

医药中间体3-醛基-4-卤代吡唑的合成方法
摘要：
本发明涉及重要医药中间体3-醛基-4-卤代(溴或碘)吡唑的合成方法。本发明的技术方案：医药中间体3-醛基-4-卤代(溴或碘)吡唑的合成方法，包括以下步骤：以2，2-二甲氧基乙醛和N，N-二甲基甲酰胺二甲基缩醛为原料生成4-二甲氨基-1，1-二甲氧基-3-丁酮；4-二甲氨基-1，1-二甲氧基-3-丁酮无需纯化直接和水合肼反应得到关键中间体3-二甲氧基甲基-1-氢吡唑；然后经过溴代或碘代，再脱保护得到3-醛基-4-溴吡唑或3-醛基-4-碘吡唑。
摘要（英）：

The present invention relates to an important pharmaceutical intermediate 3-formyl-4-halogeno (bromine or iodine) pyrazole. The technical scheme of the present invention comprises that: the synthesis method for the pharmaceutical intermediate 3-formyl-4-halogeno (bromine or iodine) pyrazole comprises the following steps that: 2,2-dimethoxy acetaldehyde and N,N-dimethylformamide dimethyl acetal are adopted as raw materials to generate 4-dimethylamino-1,1-dimethoxy-3-butanone; the 4-dimethylamino-1,1-dimethoxy-3-butanone directly reacts with hydrazine hydrate without purification to obtain a key intermediate 3-dimethoxymethyl-1-hydropyrazole; after bromination or iodo, the 3-dimethoxymethyl-1-hydropyrazole is subjected to deprotection to obtain the 3-formyl-4-bromopyrazole or 3-formyl-4-iodopyrazole.

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