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CN107021965B 一种合成5,6,7,8-四氢-1,6-萘啶-2胺的方法 有权

一种合成5,6,7,8-四氢-1,6-萘啶-2胺的方法
Abstract:
本发明公开了一种合成5,6,7,8‑四氢‑1,6‑萘啶‑2胺的方法，所述合成方法的具体步骤如下：(1)2‑卤代‑5,6,7,8‑四氢‑1,6‑萘啶经过氨基保护反应制得6位保护的2‑卤代‑5,7,8‑三氢‑1,6‑萘啶；(2)6位保护的2‑卤代‑5,7,8‑三氢‑1,6‑萘啶在碱性条件下与氨基甲酸酯，通过钯催化偶联反应制得双保护的5,7,8‑三氢‑1,6‑萘啶‑2胺；(3)双保护5,7,8‑三氢‑1,6‑萘啶‑2胺经过脱保护反应制得5,6,7,8‑四氢‑1,6‑萘啶‑2胺。本发明整个工艺过程都使用常规试剂，避免使用毒性和环境危害大的叠氮化物，反应条件温和，更加安全环保。
Abstract(English):

The invention discloses a synthesis method of 5,6,7,8-tetrahydro-1,6-naphthyridine-2-amine. The synthesis method comprises the specific steps: (1) carrying out amino protection reaction on 2-halo-5,6,7,8-tetrahydro-1,6-naphthyridine to prepare 6-site-protected 2-halo-5,7,8-trihydro-1,6-naphthyridine; (2) carrying out palladium-catalyzed coupling reaction on the 6-site-protected 2-halo-5,7,8-trihydro-1,6-naphthyridine and carbamate under basic conditionsto prepare double-site-protected 5,7,8-trihydro-1,6-naphthyridine-2-amine; (3) carrying out deprotection reaction on the double-site-protected 5,7,8-trihydro-1,6-naphthyridine-2-amine to prepare 5,6,7,8-tetrahydro-1,6-naphthyridine-2-amine. In the whole technical process, only conventional reagents are used, the use of azides with high toxicity and environmental hazards is avoided, reaction conditions are mild and the method is safer and more environmentally friendly.

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