{"id":34097,"date":"2020-08-09T08:00:32","date_gmt":"2020-08-09T00:00:32","guid":{"rendered":"\/\/www.gsbet888.com\/?p=34097"},"modified":"2020-08-03T17:43:00","modified_gmt":"2020-08-03T09:43:00","slug":"naito%e5%90%b2%e5%93%9a%e5%90%88%e6%88%90","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/reactions\/2020\/08\/naito%e5%90%b2%e5%93%9a%e5%90%88%e6%88%90.html","title":{"rendered":"Naito\u5432\u54da\u5408\u6210"},"content":{"rendered":"<h4><strong>\u6982\u8981<\/strong><\/h4>\n<p>Naito\u5432\u54da\u5408\u6210 (Naito indole synthesis)\u662f<em>N\u02b9<\/em>-\u82b3\u57fa-<em>N<\/em>-\u4e09\u6c1f\u4e59\u9170\u57fa\u70ef\u80bc (<em>N\u02b9<\/em>-aryl-<em>N<\/em>-trifluoroacetyl enehydrazine)\u5728\u52a0\u70ed\u6761\u4ef6\u4e0b\u4f9d\u6b21\u901a\u8fc7\u73af\u5316\u4ee5\u53ca\u70ed\u6d88\u9664\u53cd\u5e94\u8fc7\u7a0b\uff0c\u5f62\u6210\u5432\u54da\u7c7b\u5316\u5408\u7269\u7684\u53cd\u5e94\u3002\u8be5\u53cd\u5e94\u7531\u65e5\u672cKobe\u836f\u79d1\u5927\u5b66 (\u795e\u6238\u85ac\u79d1\u5927\u5b66, Kobe Phamaxutical University) \u7684Naito (\u5185\u85e4 \u731b\u7ae0,Naito Takeaki )\u7814\u7a76\u5ba4\u57281999\u5e74\u9996\u6b21\u62a5\u9053<sup>[1]<\/sup>\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/Naito-indole-1.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34235 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/Naito-indole-1.png\" alt=\"\" width=\"807\" height=\"600\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/Naito-indole-1.png 807w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/Naito-indole-1-300x223.png 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/Naito-indole-1-680x506.png 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/Naito-indole-1-768x571.png 768w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/Naito-indole-1-265x197.png 265w\" sizes=\"(max-width: 807px) 100vw, 807px\" \/><\/a><\/p>\n<p>2001\u5e74\uff0cNaito\u8fdb\u4e00\u6b65\u7814\u7a76\u53d1\u73b0\uff0c\u901a\u8fc7\u5404\u7c7b\u916e\u4e0e\u80bc\u4e4b\u95f4\u7684\u4e00\u9505\u53cd\u5e94\uff0c\u540c\u6837\u80fd\u591f\u987a\u5229\u5b8c\u6210\u5432\u54da\u7c7b\u5316\u5408\u7269\u7684\u5408\u6210<sup>[2]<\/sup>\u3002\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u65e0\u9700\u4e2d\u95f4\u4f53\u7684\u5206\u79bb\uff0c\u64cd\u4f5c\u7b80\u4fbf\uff0c\u5177\u6709\u826f\u597d\u7684\u6536\u7387\u4e0epot-economy<sup>[2]<\/sup>\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-36.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34099 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-36.jpg\" alt=\"\" width=\"1183\" height=\"313\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-36.jpg 1183w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-36-300x79.jpg 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-36-680x180.jpg 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-36-768x203.jpg 768w\" sizes=\"(max-width: 1183px) 100vw, 1183px\" \/><\/a><\/p>\n<p>2002\u5e74\uff0cNaito\u8fdb\u4e00\u6b65\u5c06\u5e95\u7269\u8303\u56f4\u6269\u5c55\u81f3<em>N<\/em>-\u4e09\u6c1f\u4e59\u9170\u57fa-<em>N&#8217;<\/em>-(3-\u7532\u6c27\u7fb0\u57fa\u82ef\u57fa)\u70ef\u80bc\uff0c\u5e76\u4ee5\u4e2d\u7b49\u7a0b\u5ea6\u7684\u6536\u7387\u83b7\u5f97\u76f8\u5e942,4-\u4e8c\u53d6\u4ee3\u5432\u54da\u4ea7\u7269<sup>[3]<\/sup>\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-34.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34100 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-34.jpg\" alt=\"\" width=\"631\" height=\"206\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-34.jpg 631w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-34-300x98.jpg 300w\" sizes=\"(max-width: 631px) 100vw, 631px\" \/><\/a><\/p>\n<p>2003\u5e74\uff0cNaito\u7ee7\u7eed\u5c06\u4e0a\u8ff0\u53cd\u5e94\u6761\u4ef6\u6269\u5c55\u81f3\u82ef\u5e76\u544b\u5583\u73af\u7684\u6784\u5efa\uff0c\u5e76\u83b7\u5f97\u826f\u597d\u7684\u53cd\u5e94\u6536\u7387<sup>[4]<\/sup>\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-33.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34101 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-33.jpg\" alt=\"\" width=\"1140\" height=\"817\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-33.jpg 1140w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-33-300x215.jpg 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-33-680x487.jpg 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-33-768x550.jpg 768w\" sizes=\"(max-width: 1140px) 100vw, 1140px\" \/><\/a><\/p>\n<p>Naito\u5432\u54da\u5408\u6210\u65b9\u6cd5\u5b66\u5177\u6709\u6761\u4ef6\u6e29\u548c\uff0c\u76ee\u6807\u4ea7\u7269\u4ea7\u7387\u4f18\u826f\u7b49\u4f18\u70b9\u3002\u4e3a\u5432\u54da\u73af\u7ed3\u6784\u7684\u6784\u5efa\u4ee5\u53ca\u90e8\u5206\u751f\u7269\u6d3b\u6027\u5206\u5b50\u7684\u6784\u5efa\u5f00\u8f9f\u4e86\u4e00\u79cd\u66f4\u4e3a\u7b80\u4fbf\u7684\u65b9\u6cd5<sup>[5]-[6]<\/sup>\u3002<\/p>\n<h4><strong>\u57fa\u672c\u6587\u732e<\/strong><\/h4>\n<ul>\n<li>[1] O. Miyata, Y. Kimura, K. Muroya, H. Hiramatsu, T. Naito, Tetrahedron Lett. 1999, 40, 3601. doi: <a href=\"https:\/\/doi.org\/10.1016\/S0040-4039(99)00583-3\">10.1016\/S0040-4039(99)00583-3<\/a>.<\/li>\n<li>[2] O. Miyata, Y. Kimura, T. Naito, Synthesis, 2001, 1635. doi:<a href=\"https:\/\/www.thieme-connect.de\/products\/ejournals\/abstract\/10.1055\/s-2001-16756\"> 10.1055\/s-2001-16756.<\/a><\/li>\n<li>[3] O. Miyata, N. Takeda, T. Naito, Heterocycles 2002, 57, 1101. doi: <a href=\"https:\/\/www.heterocycles.jp\/newlibrary\/libraries\/abst\/00717\">10.3987\/COM-02-9476.<\/a><\/li>\n<li>[4] O. Miyata, N. Takeda, Y. Morikami, T. Naito, Org. Biomol. Chem. 2003, 1, 254. doi: <a href=\"https:\/\/doi.org\/10.1039\/B210059B\">10.1039\/B210059B<\/a>.<\/li>\n<li>[5] O. Miyata, N. Takeda, Y. Kimura, Y. Takemoto, N. Tohnai, M. Miyata, T. Naito, Tetrahedron 2006, 62, 3629. doi: <a href=\"https:\/\/doi.org\/10.1016\/j.tet.2006.01.087\">10.1016\/j.tet.2006.01.087<\/a>.<\/li>\n<li>[6] O. Miyata, N. Takeda, T. Naito, Org. Lett. 2004, 6, 1761. doi: <a href=\"https:\/\/pubs.acs.org\/doi\/10.1021\/ol049564o\">10.1021\/ol049564o.<\/a><\/li>\n<\/ul>\n<h4><strong>\u53cd\u5e94\u673a\u7406<\/strong><\/h4>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-25.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34102 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-25.jpg\" alt=\"\" width=\"1197\" height=\"950\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-25.jpg 1197w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-25-300x238.jpg 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-25-680x540.jpg 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-25-768x610.jpg 768w\" sizes=\"(max-width: 1197px) 100vw, 1197px\" \/><\/a><\/p>\n<h4>\u53c2<strong>\u8003\u6587\u732e<\/strong><\/h4>\n<ul>\n<li>[1] O. Miyata, Y. Kimura, T. Naito, Chem. Commun. 1999, 2429. doi: <a href=\"https:\/\/doi.org\/10.1039\/A907539I\">10.1039\/A907539I<\/a>.<\/li>\n<li>[2] O. Miyata, N. Takeda, Y. Kimura, Y. Takemoto, N. Tohnai, M. Miyata, T. Naito, Tetrahedron 2006, 62, 3629. doi: <a href=\"https:\/\/doi.org\/10.1016\/j.tet.2006.01.087\">10.1016\/j.tet.2006.01.087<\/a>.<\/li>\n<li>[3] O. Miyata, N. Takeda, Y. Kimura, Y. Takemoto, N. Tohnai, M. Miyata, T. Naito, Tetrahedron 2006, 62, 3629. doi: <a href=\"https:\/\/doi.org\/10.1016\/j.tet.2006.01.087\">10.1016\/j.tet.2006.01.087<\/a>.<\/li>\n<\/ul>\n<h4><strong>\u53cd\u5e94\u5b9e\u4f8b<\/strong><\/h4>\n<p>\u5432\u54da\u7684\u5408\u6210<sup>[1]<\/sup><\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/6-20.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34103 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/6-20.jpg\" alt=\"\" width=\"612\" height=\"170\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/6-20.jpg 612w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/6-20-300x83.jpg 300w\" sizes=\"(max-width: 612px) 100vw, 612px\" \/><\/a><\/p>\n<p>\u82ef\u5e76\u544b\u5583\u7684\u5408\u6210<sup>[2]<\/sup><\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/7-17.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34104 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/7-17.jpg\" alt=\"\" width=\"638\" height=\"156\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/7-17.jpg 638w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/7-17-300x73.jpg 300w\" sizes=\"(max-width: 638px) 100vw, 638px\" \/><\/a><\/p>\n<p>eupomatenoid 6\u7684\u5408\u6210<sup>[3]<\/sup><\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/8-17.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34109 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/8-17.jpg\" alt=\"\" width=\"953\" height=\"411\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/8-17.jpg 953w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/8-17-300x129.jpg 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/8-17-680x293.jpg 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/8-17-768x331.jpg 768w\" sizes=\"(max-width: 953px) 100vw, 953px\" \/><\/a><\/p>\n<h4><strong>\u5b9e\u9a8c\u6b65\u9aa4<\/strong><\/h4>\n<p>\u5c06<em>N\u02b9<\/em>-\u82b3\u57fa-<em>N<\/em>-\u4e09\u6c1f\u4e59\u9170\u57fa\u70ef\u80bc\u6eb6\u4e8e\u9002\u91cf\u7532\u82ef (\u7ef4\u6301\u5e95\u7269\u6d53\u5ea6\u4e3a0.008 M)\u4e2d\u3002\u5c06\u4e0a\u8ff0\u5747\u76f8\u6df7\u5408\u7269\u52a0\u70ed\u56de\u6d41\uff0c\u5e76\u901a\u8fc7TLC\u76d1\u63a7\uff0c\u76f4\u81f3\u53cd\u5e94\u7ed3\u675f\u3002\u53cd\u5e94\u7ed3\u675f\u540e\uff0c\u5c06\u4e0a\u8ff0\u6df7\u5408\u7269\u51cf\u538b\u6d53\u7f29\u3002\u6b8b\u4f59\u7269\u901a\u8fc7MPCC (medium-pressure column chromatography)\u8fdb\u884c\u5206\u79bb\u7eaf\u5316 (\u6b63\u5df1\u70f7\/\u4e59\u9178\u4e59\u916f 5 : 1 v\/v \u4f5c\u4e3a\u6d17\u8131\u5242), \u83b7\u5f97\u76f8\u5e94\u5432\u54da\u4ea7\u7269\u3002<\/p>\n<h4><strong>\u53c2\u8003\u6587\u732e<\/strong><\/h4>\n<ul>\n<li>[1] O. Miyata, Y. Kimura, K. Muroya, H. Hiramatsu, T. Naito, Tetrahedron Lett. 1999, 40, 3601. doi: <a href=\"https:\/\/doi.org\/10.1016\/S0040-4039(99)00583-3\">10.1016\/S0040-4039(99)00583-3<\/a>.<\/li>\n<li>[2] O. Miyata, N. Takeda, Y. Morikami, T. Naito, Org. Biomol. Chem. 2003, 1, 254. doi: <a href=\"https:\/\/doi.org\/10.1039\/B210059B\">10.1039\/B210059B<\/a>.<\/li>\n<li>[3] O. Miyata, N. Takeda, T. Naito, Org. Lett. 2004, 6, 1761. doi: <a href=\"https:\/\/pubs.acs.org\/doi\/10.1021\/ol049564o\">10.1021\/ol049564o.<\/a><\/li>\n<\/ul>\n<p>\u672c\u6587\u7248\u6743\u5c5e\u4e8e<strong>\u00a0<a href=\"\/\/www.gsbet888.com\/\">Chem-Station\u5316\u5b66\u7a7a\u95f4<\/a>\uff0c<\/strong>\u00a0\u6b22\u8fce\u70b9\u51fb\u6309\u94ae\u5206\u4eab\uff0c\u672a\u7ecf\u8bb8\u53ef\uff0c\u8c22\u7edd\u8f6c\u8f7d\uff01<\/p>\n","protected":false},"excerpt":{"rendered":"\u6982\u8981 Naito\u5432\u54da\u5408\u6210 (Naito indole synthesis)\u662fN\u02b9-\u82b3\u57fa-N-\u4e09\u6c1f\u4e59\u9170\u57fa\u70ef\u80bc (N\u02b9-aryl-N-trifluoroacetyl enehydrazine)\u5728\u52a0\u70ed\u6761\u4ef6\u4e0b\u4f9d\u6b21\u901a\u8fc7\u73af\u5316\u4ee5\u53ca\u70ed\u6d88\u9664\u53cd\u5e94\u8fc7\u7a0b\uff0c\u5f62\u6210\u5432\u54da\u7c7b\u5316\u5408\u7269\u7684\u53cd\u5e94\u3002\u8be5\u53cd\u5e94\u7531\u65e5\u672cKobe\u836f\u79d1\u5927\u5b66 (\u795e\u6238\u85ac\u79d1\u5927\u5b66, Kobe Phamaxutical University) \u7684Naito (\u5185\u85e4 \u731b\u7ae0,Naito Takeaki )\u7814\u7a76\u5ba4\u57281999\u5e74\u9996\u6b21\u62a5\u9053[1]\u3002 2001\u5e74\uff0cNaito\u8fdb\u4e00\u6b65\u7814\u7a76\u53d1\u73b0\uff0c\u901a\u8fc7\u5404\u7c7b\u916e\u4e0e\u80bc\u4e4b\u95f4\u7684\u4e00\u9505\u53cd\u5e94\uff0c\u540c\u6837\u80fd\u591f\u987a\u5229\u5b8c\u6210\u5432\u54da\u7c7b\u5316\u5408\u7269\u7684\u5408\u6210[2]\u3002\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u65e0\u9700\u4e2d\u95f4\u4f53\u7684\u5206\u79bb\uff0c\u64cd\u4f5c\u7b80\u4fbf\uff0c\u5177\u6709\u826f\u597d\u7684\u6536\u7387\u4e0epot-economy[2]\u3002 2002\u5e74\uff0cNaito\u8fdb\u4e00\u6b65\u5c06\u5e95\u7269\u8303\u56f4\u6269\u5c55\u81f3N-\u4e09\u6c1f\u4e59\u9170\u57fa-N&#8217;-(3-\u7532\u6c27\u7fb0\u57fa\u82ef\u57fa)\u70ef\u80bc\uff0c\u5e76\u4ee5\u4e2d\u7b49\u7a0b\u5ea6\u7684\u6536\u7387\u83b7\u5f97\u76f8\u5e942,4-\u4e8c\u53d6\u4ee3\u5432\u54da\u4ea7\u7269[3]\u3002 2003\u5e74\uff0cNaito\u7ee7\u7eed\u5c06\u4e0a\u8ff0\u53cd\u5e94\u6761\u4ef6\u6269\u5c55\u81f3\u82ef\u5e76\u544b\u5583\u73af\u7684\u6784\u5efa\uff0c\u5e76\u83b7\u5f97\u826f\u597d\u7684\u53cd\u5e94\u6536\u7387[4]\u3002 Naito\u5432\u54da\u5408\u6210\u65b9\u6cd5\u5b66\u5177\u6709\u6761\u4ef6\u6e29\u548c\uff0c\u76ee\u6807\u4ea7\u7269\u4ea7\u7387\u4f18\u826f\u7b49\u4f18\u70b9\u3002\u4e3a\u5432\u54da\u73af\u7ed3\u6784\u7684\u6784\u5efa\u4ee5\u53ca\u90e8\u5206\u751f\u7269\u6d3b\u6027\u5206\u5b50\u7684\u6784\u5efa\u5f00\u8f9f\u4e86\u4e00\u79cd\u66f4\u4e3a\u7b80\u4fbf\u7684\u65b9\u6cd5[5]-[6]\u3002 \u57fa\u672c\u6587\u732e [1] O. Miyata, Y. Kimura, K. Muroya, H. Hiramatsu, T. Naito, Tetrahedron Lett. 1999, 40, 3601. doi: 10.1016\/S0040-4039(99)00583-3. [2] O. Miyata, Y. Kimura, T. Naito, Synthesis, 2001, 1635. doi: 10.1055\/s-2001-16756. [3] O. Miyata, N. Takeda, T. Naito, Heterocycles 2002, 57, 1101. doi: 10.3987\/COM-02-9476. [4] O. Miyata, N. Takeda, Y. Morikami, T. Naito, Org. Biomol. Chem. 2003, 1, 254. doi: 10.1039\/B210059B. [5] O. Miyata, N. Takeda, Y. Kimura, Y. Takemoto, N. Tohnai, M. Miyata, T. Naito, Tetrahedron 2006, 62, 3629. doi: 10.1016\/j.tet.2006.01.087. [6] O. Miyata, N. Takeda, T. Naito, Org. 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