Synthesis method of 1H-benzo [f] indole

The invention discloses a synthesis method of 1H-benzo [f] indole, which comprises the following steps: (1) carrying out amino protection reaction on 2-aminonaphthalene and di-tert-butyl dicarbonate ester under a heating condition to obtain N-Boc-2-aminonaphthalene; (2) carrying out electrophilic su...

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Bibliographische Detailangaben
Hauptverfasser: LI WEIJUN, ZHANG CHENG, CHEN JIAN'AI, TAN SIJIE
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a synthesis method of 1H-benzo [f] indole, which comprises the following steps: (1) carrying out amino protection reaction on 2-aminonaphthalene and di-tert-butyl dicarbonate ester under a heating condition to obtain N-Boc-2-aminonaphthalene; (2) carrying out electrophilic substitution reaction and deamination protection reaction on the N-Boc-2-aminonaphthalene, so as to obtain 2-amino-3-iodonaphthalene; (3) carrying out reaction on the 2-amino-3-iodonaphthalene and trimethylsilyl acetylene in the presence of a catalyst under an alkaline condition, so as to obtain 2-amino-3-(trimethylsilyl) ethynyl naphthalene; (4) the 2-amino-3-(trimethylsilyl) ethynyl naphthalene is subjected to a reaction under the alkaline condition, and 2-amino-3-ethynyl naphthalene is obtained; and (5) catalyzing the 2-amino-3-ethynyl naphthalene under the catalysis of the transition metal complex to obtain the target product 1H-benzo [f] indole. The whole preparation process is environment-friendly and pollution