{"id":34088,"date":"2020-08-02T16:39:15","date_gmt":"2020-08-02T08:39:15","guid":{"rendered":"\/\/www.gsbet888.com\/?p=34088"},"modified":"2020-08-02T16:53:27","modified_gmt":"2020-08-02T08:53:27","slug":"kihara-%e5%90%b2%e5%93%9a%e5%90%88%e6%88%90","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/reactions\/2020\/08\/kihara-%e5%90%b2%e5%93%9a%e5%90%88%e6%88%90.html","title":{"rendered":"Kihara \u5432\u54da\u5408\u6210"},"content":{"rendered":"<h4><strong>\u6982\u8981<\/strong><\/h4>\n<p>Kihara\u5432\u54da\u5408\u6210 (Kihara indole synthesis)\u662f\u901a\u8fc7\u5f3a\u78b1(\u6b63\u4e01\u57fa\u9502)\u6761\u4ef6\u4e0b\u539f\u4f4d\u751f\u6210\u7684\u82b3\u57fa\u9502\u8bd5\u5242\u8fdb\u884c\u7684\u5206\u5b50\u5185Barbier\u53cd\u5e94\uff0c\u8fdb\u800c\u5b8c\u6210\u76841-\u7532\u57fa-3-\u82b3\u57fa\u5432\u54da\u4e0e1-\u7532\u57fa-3-\u70f7\u57fa\u5432\u54da\u53ca1-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7684\u5408\u6210<sup>[1]<\/sup>\u3002\u8be5\u53cd\u5e94\u7531\u65e5\u672cTokushima\u5927\u5b66\u836f\u5b66\u90e8\u7684Kihara (\u6728\u539f \u52dd, \u5fb3\u5cf6\u5927\u5b66\u85ac\u5b66\u90e8, Kihara Masaru, Faculty of Pharmaceutical Sciences, The University of Tokushima) \u57281995\u5e74\u9996\u6b21\u62a5\u9053\u3002\u8be5\u65b9\u6cd5\u5b66\u539f\u6599\u6613\u5f97\uff0c\u4ea7\u7387\u4e2d\u7b49\uff0c\u4e3a1-\u7532\u57fa-3-\u82b3\u57fa\u5432\u54da\u4e0e1-\u7532\u57fa-3-\u70f7\u57fa\u5432\u54da\u53ca1-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7684\u5408\u6210\u5f00\u8f9f\u4e86\u65b0\u7684\u9014\u5f84\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/kuhara1.png\"><img loading=\"lazy\" decoding=\"async\" class=\"alignleft size-large wp-image-34217\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/kuhara1-680x231.png\" alt=\"\" width=\"680\" height=\"231\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/kuhara1-680x231.png 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/kuhara1-300x102.png 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/kuhara1-768x261.png 768w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/kuhara1.png 852w\" sizes=\"(max-width: 680px) 100vw, 680px\" \/><\/a><\/p>\n<h4><strong>\u57fa\u672c\u6587\u732e<\/strong><\/h4>\n<ul>\n<li>[1] M. Kihara, Y. Iwai, Y. Nagao, Heterocycles, 1995, 41, 2279. doi <a href=\"https:\/\/www.heterocycles.jp\/newlibrary\/libraries\/abst\/06026\">10.3987\/COM-95-7177.<\/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\/2-35.jpg\"><br \/>\n<img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34090 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-35.jpg\" alt=\"\" width=\"1121\" height=\"680\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-35.jpg 1121w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-35-300x182.jpg 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-35-680x412.jpg 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-35-768x466.jpg 768w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/2-35-660x400.jpg 660w\" sizes=\"(max-width: 1121px) 100vw, 1121px\" \/><\/a><\/p>\n<h4><strong>\u53cd\u5e94\u5b9e\u4f8b<\/strong><\/h4>\n<p>1-\u7532\u57fa-3-\u82b3\u57fa\u5432\u54da\u7684\u5408\u6210<sup>[1]<\/sup><\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-33.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34091 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-33.jpg\" alt=\"\" width=\"717\" height=\"181\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-33.jpg 717w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-33-300x76.jpg 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/3-33-680x172.jpg 680w\" sizes=\"(max-width: 717px) 100vw, 717px\" \/><\/a><\/p>\n<p>1-\u7532\u57fa-3-\u70f7\u57fa\u5432\u54da\u7684\u5408\u6210<sup>[1]<\/sup><\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-32.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34092 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-32.jpg\" alt=\"\" width=\"679\" height=\"182\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-32.jpg 679w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/4-32-300x80.jpg 300w\" sizes=\"(max-width: 679px) 100vw, 679px\" \/><\/a><\/p>\n<p>1-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7684\u5408\u6210<sup>[1]<\/sup><\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-24.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-34093 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-24.jpg\" alt=\"\" width=\"933\" height=\"497\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-24.jpg 933w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-24-300x160.jpg 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-24-680x362.jpg 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/5-24-768x409.jpg 768w\" sizes=\"(max-width: 933px) 100vw, 933px\" \/><\/a><\/p>\n<h4><strong>\u5b9e\u9a8c\u6b65\u9aa4<\/strong><\/h4>\n<p><span style=\"color: #0000ff\"><strong>1. Kihara<\/strong><strong>\u5432\u54da\u5408\u6210<\/strong><\/span><\/p>\n<p>\u5728-78 <sup>o<\/sup>C\uff0c\u6c2e\u6c14\u6c14\u6c1b\u4e0b\uff0c\u5c06\u6b63\u4e01\u57fa\u9502 (l.6 M \u6b63\u5df1\u70f7\u6eb6\u6db2\uff0c1.2 eq.)\u7f13\u6162\u6ef4\u52a0\u81f3<em>N<\/em>-(2-\u7898\u82ef\u57fa)-<em>N<\/em>-\u7532\u6c28\u57fa\u7532\u57fa\u916e (1 eq.)\u7684\u65e0\u6c34\u56db\u6c22\u544b\u5583\u6eb6\u6db2 (\u5e95\u7269\u6d53\u5ea6\u4e3a0.11 M)\u4e2d\u3002\u7ef4\u6301-78 <sup>o<\/sup>C\uff0c\u5c06\u4e0a\u8ff0\u53cd\u5e94\u6df7\u5408\u7269\u6405\u62cc15 min\u300215 min\u540e\uff0c\u52a0\u5165\u6c34\u6dec\u706d\u53cd\u5e94\u3002\u6dec\u706d\u5b8c\u6210\u540e\uff0c\u518d\u52a0\u5165\u4e59\u919a\u8fdb\u884c\u8403\u53d6\u3002\u5c06\u5408\u5e76\u7684\u6709\u673a\u76f8\u901a\u8fc7\u65e0\u6c34\u786b\u9178\u9541\u5e72\u71e5\u540e\uff0c\u51cf\u538b\u9664\u53bb\u6eb6\u5242\u3002\u7c97\u4ea7\u7269\u9996\u5148\u901a\u8fc7\u7845\u80f6\u5feb\u901f\u67f1\u8272\u8c31 (DCM\u4f5c\u4e3a\u6d17\u8131\u5242)\u5206\u79bb\u51fa\u76f8\u5e941-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7ec4\u5206\uff0c\u968f\u540e\u5c06\u8be5\u7ec4\u5206\u7ee7\u7eed\u901a\u8fc7\u7845\u80f6\u5feb\u901f\u67f1\u8272\u8c31 (DCM\/\u6b63\u5df1\u70f7 1:1v\/v \u4f5c\u4e3a\u6d17\u8131\u5242)\u8fdb\u884c\u7eaf\u5316\uff0c\u83b7\u5f97\u76f8\u5e94\u5432\u54da\u4ea7\u7269\u3002<\/p>\n<p><span style=\"color: #0000ff\"><strong>2. \u5728<\/strong><strong>HCl\/Et<sub>2<\/sub>O<\/strong><strong>\u6761\u4ef6\u4e0b\u7684\u8131\u6c34<\/strong><\/span><\/p>\n<p>\u54111-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u62161-\u7532\u57fa-3-\u82ef\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7684\u4e59\u919a\u6eb6\u6db2\u4e2d\u52a0\u5165\u9002\u91cf5% HCl\u6eb6\u6db2\u3002\u518d\u5c06\u4e0a\u8ff0\u6df7\u5408\u7269\u5728\u5ba4\u6e29\u4e0b\u6405\u62cc10 min\u3002\u4e4b\u540e\uff0c\u52a0\u5165\u9002\u91cf10% KOH\u8fdb\u884c\u4e2d\u548c\uff0c\u968f\u540e\uff0c\u52a0\u5165DCM\u8fdb\u884c\u8403\u53d6\u3002\u5c06\u5408\u5e76\u7684\u6709\u673a\u76f8\u52a0\u6c34\u6d17\u6da4\uff0c\u518d\u901a\u8fc7\u65e0\u6c34\u786b\u9178\u9541\u8fdb\u884c\u5e72\u71e5\u3002\u51cf\u538b\u9664\u53bb\u6eb6\u5242\u540e\uff0c\u83b7\u5f97\u76f8\u5e94\u5432\u54da\u4ea7\u7269\u3002<\/p>\n<h4><strong>\u53c2\u8003\u6587\u732e<\/strong><\/h4>\n<ul>\n<li>[1] M. Kihara, Y. Iwai, Y. Nagao, Heterocycles, 1995, 41, 2279. doi <a href=\"https:\/\/www.heterocycles.jp\/newlibrary\/libraries\/abst\/06026\">10.3987\/COM-95-7177.<\/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 Kihara\u5432\u54da\u5408\u6210 (Kihara indole synthesis)\u662f\u901a\u8fc7\u5f3a\u78b1(\u6b63\u4e01\u57fa\u9502)\u6761\u4ef6\u4e0b\u539f\u4f4d\u751f\u6210\u7684\u82b3\u57fa\u9502\u8bd5\u5242\u8fdb\u884c\u7684\u5206\u5b50\u5185Barbier\u53cd\u5e94\uff0c\u8fdb\u800c\u5b8c\u6210\u76841-\u7532\u57fa-3-\u82b3\u57fa\u5432\u54da\u4e0e1-\u7532\u57fa-3-\u70f7\u57fa\u5432\u54da\u53ca1-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7684\u5408\u6210[1]\u3002\u8be5\u53cd\u5e94\u7531\u65e5\u672cTokushima\u5927\u5b66\u836f\u5b66\u90e8\u7684Kihara (\u6728\u539f \u52dd, \u5fb3\u5cf6\u5927\u5b66\u85ac\u5b66\u90e8, Kihara Masaru, Faculty of Pharmaceutical Sciences, The University of Tokushima) \u57281995\u5e74\u9996\u6b21\u62a5\u9053\u3002\u8be5\u65b9\u6cd5\u5b66\u539f\u6599\u6613\u5f97\uff0c\u4ea7\u7387\u4e2d\u7b49\uff0c\u4e3a1-\u7532\u57fa-3-\u82b3\u57fa\u5432\u54da\u4e0e1-\u7532\u57fa-3-\u70f7\u57fa\u5432\u54da\u53ca1-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7684\u5408\u6210\u5f00\u8f9f\u4e86\u65b0\u7684\u9014\u5f84\u3002 \u57fa\u672c\u6587\u732e [1] M. Kihara, Y. Iwai, Y. Nagao, Heterocycles, 1995, 41, 2279. doi 10.3987\/COM-95-7177. \u53cd\u5e94\u673a\u7406 \u53cd\u5e94\u5b9e\u4f8b 1-\u7532\u57fa-3-\u82b3\u57fa\u5432\u54da\u7684\u5408\u6210[1] 1-\u7532\u57fa-3-\u70f7\u57fa\u5432\u54da\u7684\u5408\u6210[1] 1-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7684\u5408\u6210[1] \u5b9e\u9a8c\u6b65\u9aa4 1. Kihara\u5432\u54da\u5408\u6210 \u5728-78 oC\uff0c\u6c2e\u6c14\u6c14\u6c1b\u4e0b\uff0c\u5c06\u6b63\u4e01\u57fa\u9502 (l.6 M \u6b63\u5df1\u70f7\u6eb6\u6db2\uff0c1.2 eq.)\u7f13\u6162\u6ef4\u52a0\u81f3N-(2-\u7898\u82ef\u57fa)-N-\u7532\u6c28\u57fa\u7532\u57fa\u916e (1 eq.)\u7684\u65e0\u6c34\u56db\u6c22\u544b\u5583\u6eb6\u6db2 (\u5e95\u7269\u6d53\u5ea6\u4e3a0.11 M)\u4e2d\u3002\u7ef4\u6301-78 oC\uff0c\u5c06\u4e0a\u8ff0\u53cd\u5e94\u6df7\u5408\u7269\u6405\u62cc15 min\u300215 min\u540e\uff0c\u52a0\u5165\u6c34\u6dec\u706d\u53cd\u5e94\u3002\u6dec\u706d\u5b8c\u6210\u540e\uff0c\u518d\u52a0\u5165\u4e59\u919a\u8fdb\u884c\u8403\u53d6\u3002\u5c06\u5408\u5e76\u7684\u6709\u673a\u76f8\u901a\u8fc7\u65e0\u6c34\u786b\u9178\u9541\u5e72\u71e5\u540e\uff0c\u51cf\u538b\u9664\u53bb\u6eb6\u5242\u3002\u7c97\u4ea7\u7269\u9996\u5148\u901a\u8fc7\u7845\u80f6\u5feb\u901f\u67f1\u8272\u8c31 (DCM\u4f5c\u4e3a\u6d17\u8131\u5242)\u5206\u79bb\u51fa\u76f8\u5e941-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7ec4\u5206\uff0c\u968f\u540e\u5c06\u8be5\u7ec4\u5206\u7ee7\u7eed\u901a\u8fc7\u7845\u80f6\u5feb\u901f\u67f1\u8272\u8c31 (DCM\/\u6b63\u5df1\u70f7 1:1v\/v \u4f5c\u4e3a\u6d17\u8131\u5242)\u8fdb\u884c\u7eaf\u5316\uff0c\u83b7\u5f97\u76f8\u5e94\u5432\u54da\u4ea7\u7269\u3002 2. \u5728HCl\/Et2O\u6761\u4ef6\u4e0b\u7684\u8131\u6c34 \u54111-\u7532\u57fa-3-\u70f7\u57fa-3-\u7f9f\u57fa\u5432\u54da\u62161-\u7532\u57fa-3-\u82ef\u57fa-3-\u7f9f\u57fa\u5432\u54da\u7684\u4e59\u919a\u6eb6\u6db2\u4e2d\u52a0\u5165\u9002\u91cf5% HCl\u6eb6\u6db2\u3002\u518d\u5c06\u4e0a\u8ff0\u6df7\u5408\u7269\u5728\u5ba4\u6e29\u4e0b\u6405\u62cc10 min\u3002\u4e4b\u540e\uff0c\u52a0\u5165\u9002\u91cf10% KOH\u8fdb\u884c\u4e2d\u548c\uff0c\u968f\u540e\uff0c\u52a0\u5165DCM\u8fdb\u884c\u8403\u53d6\u3002\u5c06\u5408\u5e76\u7684\u6709\u673a\u76f8\u52a0\u6c34\u6d17\u6da4\uff0c\u518d\u901a\u8fc7\u65e0\u6c34\u786b\u9178\u9541\u8fdb\u884c\u5e72\u71e5\u3002\u51cf\u538b\u9664\u53bb\u6eb6\u5242\u540e\uff0c\u83b7\u5f97\u76f8\u5e94\u5432\u54da\u4ea7\u7269\u3002 \u53c2\u8003\u6587\u732e [1] M. Kihara, Y. Iwai, Y. Nagao, Heterocycles, 1995, 41, 2279. doi 10.3987\/COM-95-7177. \u672c\u6587\u7248\u6743\u5c5e\u4e8e\u00a0Chem-Station\u5316\u5b66\u7a7a\u95f4\uff0c\u00a0\u6b22\u8fce\u70b9\u51fb\u6309\u94ae\u5206\u4eab\uff0c\u672a\u7ecf\u8bb8\u53ef\uff0c\u8c22\u7edd\u8f6c\u8f7d\uff01","protected":false},"author":21,"featured_media":34094,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"jetpack_post_was_ever_published":false,"_jetpack_newsletter_access":"","_jetpack_dont_email_post_to_subs":false,"_jetpack_newsletter_tier_id":0,"_jetpack_memberships_contains_paywalled_content":false,"_jetpack_memberships_contains_paid_content":false,"footnotes":"","jetpack_publicize_message":"","jetpack_publicize_feature_enabled":true,"jetpack_social_post_already_shared":true,"jetpack_social_options":{"image_generator_settings":{"template":"highway","enabled":false},"version":2}},"categories":[2],"tags":[1807,114,2947],"jetpack_publicize_connections":[],"jetpack_featured_media_url":"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/07\/Kihara-indole-synthesis.png","jetpack_shortlink":"https:\/\/wp.me\/p96op1-8RO","jetpack_sharing_enabled":true,"_links":{"self":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/34088"}],"collection":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/users\/21"}],"replies":[{"embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/comments?post=34088"}],"version-history":[{"count":8,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/34088\/revisions"}],"predecessor-version":[{"id":34223,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/34088\/revisions\/34223"}],"wp:featuredmedia":[{"embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/media\/34094"}],"wp:attachment":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/media?parent=34088"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/categories?post=34088"},{"taxonomy":"post_tag","embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/tags?post=34088"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}