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发明公开
CN106957255A 一种(R)‑N‑Boc‑5‑溴‑1‑甲基异吲哚啉及其制备方法和应用 有权 许可

一种(R)‑N‑Boc‑5‑溴‑1‑甲基异吲哚啉及其制备方法和应用
摘要：
本发明提供了一种(R)‑N‑Boc‑5‑溴‑1‑甲基异吲哚啉及其制备方法和应用，(R)‑4‑溴‑α‑苯乙胺在路易斯酸作用下与多聚甲醛反应，得到(R)‑5‑溴‑1‑甲基异吲哚啉，进而利用叔丁氧羰基对仲氨基进行保护得到(R)‑N‑Boc‑5‑溴‑1‑甲基异吲哚啉，该成环方法步骤新颖独特，易于操作，收率较高。利用拆分试剂首先拆分得到手性的制备原料(R)‑4‑溴‑α‑苯乙胺，进而制备得到(R)‑5‑溴‑1‑甲基异吲哚啉，使得可以大大缩减了体量，使体量大幅减小，整个过程的拆分浪费也大幅减小。本发明的整个制备方法的原料易得，工艺操作简单、成本低，具有较高的实际应用价值。
摘要（英）：

The invention provides (R)-N-Boc-5-bromine-1-methylisoindoline as well as a preparation method and application thereof. Reaction between (R)-4-bromine-phenylethylamine and paraformaldehyde is carried out under an effect of Lewis acid to obtain the (R)-5-bromine-1-methylisoindoline; and a secondary amino group is protected by further utilizing butoxycarbonyl to obtain the (R)-N-Boc-5-bromine-1-methylisoindoline. The cyclization method comprises novel and unique steps, is easy to operate and relatively high in yield. The splitting is carried out firstly by utilizing splitting reagent to obtain the chirally-prepared (R)-4-bromine-phenylethylamine raw material so as to further prepare the (R)-5-bromine-1-methylisoindoline, thereby greatly reducing volumes; and the volumes are greatly reduced, and splitting wastes in the whole process also can be reduced. The whole preparation method disclosed by the invention has easily-available raw materials, is simple in process operation and low in cost and has a relatively practical application value.

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