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CN105968049A 一种制备1-(2,6-二氯苄基-3-（吡咯烷-1-甲基）-6-氨基吲唑的方法 无效 - 驳回

一种制备1-(2,6-二氯苄基-3-（吡咯烷-1-甲基）-6-氨基吲唑的方法
摘要：
本发明提供一种制备1‑(2,6‑二氯苄基‑3‑(吡咯烷‑1‑甲基)‑6‑氨基吲唑(以下简称TM)的方法，包括如下步骤：步骤1：由起始原料6‑硝基吲哚啉经过酸性亚硝酸盐反应生成吲唑中间体I；步骤2：中间体I在碱性条件下和2，6‑二氯苄溴生成中间体II；步骤3：中间体II和吡咯烷生成烯胺直接原位用还原剂还原成中间体III；步骤4：中间体III的硝基还原成氨基得到目标产物TM。本发明提供的TM制备方法，不但避免了副产物化合物3的产生，而且提高了产率，还简化了纯化方法。
摘要（英）：

The invention provides a method for preparing 1-(2,6-dichlorobenzyl-3-(pyrrolidine-1-methyl)-6-aminoindazole. The method comprises the following steps: Step 1, a starting material 6-nitroindoline reacts with acidic nitrite to generate an indazole intermediate I; Step 2, the intermediate I reacts with 2,6-dichlorobenzylbromide under an alkaline condition to generate an intermediate II; Step 3, the intermediate II and pyrrolidine react to generate enamine, and enamine directly undergoes in-situ reduction to obtain an intermediate III; and Step 4, a nitro group of the intermediate III is reduced into an amino group so as to obtain the target product TM. By the TM preparation method provided by the invention, generation of a by-product compound 3 is avoided, yield is increased, and a purification method is simplified.

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