1981\u5e74\u5f00\u59cb\uff0c\u65e5\u672c\u76f8\u6a21\u5316\u5b66\u7814\u7a76\u4e2d\u5fc3 (\u76f8\u6a21\u4e2d\u592e\u5316\u5b66\u7814\u7a76\u6240, Sagami Chemical Research Center)\u7684\u5c3e\u5c9b\u4e25 (\u5c3e\u5cf6 \u5dcc\uff0c<\/a>Ojima Iwao) \u7814\u7a76\u7ec4\u8fdb\u4e00\u6b65\u5c06\u4e0d\u5bf9\u79f0Staudinger\u70ef\u916e-\u4e9a\u80fa[2+2]\u73af\u52a0\u6210 (asymmetric Staudinger ketene-imine [2+2] cycloaddition)[1]-[4]<\/sup>\u53caStaudinger\u4e0d\u5bf9\u79f0\u916f\u70ef\u9187\u8d1f\u79bb\u5b50-\u4e9a\u80fa\u73af\u7f29\u5408 (Staudinger asymmetric ester enolate-imine cyclocondensation)[5]-[7]<\/sup>\u5e94\u7528\u4e8e\u5404\u79cd\u624b\u6027\u03b2-\u5185\u9170\u80fa\u7c7b\u5316\u5408\u7269\u7684\u6784\u5efa[1]-[7]<\/sup>\u3002<\/p>\n
\u6c28\u57fa\u9178\u53ca\u5176\u884d\u751f\u7269\u7684\u5408\u6210[1]<\/sup><\/p>\n
\u6742\u73af\u5316\u5408\u7269\u7684\u5408\u6210[2]<\/sup><\/p>\n
\u70ef\u916e-\u4e9a\u80fa<\/strong>[2+2]<\/strong>\u73af\u52a0\u6210<\/strong><\/p>\n
\u5411\u5706\u5e95\u70e7\u74f6\u4e2d\u52a0\u5165\u4e9a\u80fa (1 eq.)\uff0c\u4e4b\u540e\u52a0\u5165\u65e0\u6c34THF\u6eb6\u89e3 (\u7ef4\u6301\u5e95\u7269\u6d53\u5ea6\u4e3a0.4 M)\uff0c\u968f\u540e\uff0c\u52a0\u5165\u4e09\u4e59\u80fa (3 eq.)\u3002\u5c06\u4e0a\u8ff0\u6df7\u5408\u7269\u51b7\u5374\u81f30 \u00b0C\uff0c\u968f\u540e\u6ef4\u52a0\u9170\u6c2f\u7684\u65e0\u6c34THF\u6eb6\u6db2 (1.5eq., \u9170\u6c2f\u6d53\u5ea6\u4e3a2.5 M)\u3002\u6ef4\u52a0\u7ed3\u675f\u540e\uff0c\u5347\u81f3\u5ba4\u6e29\uff0c\u5c06\u4e0a\u8ff0\u53cd\u5e94\u6df7\u5408\u7269\u5728\u5ba4\u6e29\u4e0b\u8fdb\u884c\u6405\u62cc\uff0c\u76f4\u81f3\u53cd\u5e94\u7ed3\u675f\u3002\u53cd\u5e94\u7ed3\u675f\u540e\uff0c\u51cf\u538b\u9664\u53bb\u6eb6\u5242\u3002\u5c06\u6b8b\u4f59\u7269\u901a\u8fc7\u4e8c\u6c2f\u7532\u70f7\u6eb6\u89e3\uff0c\u52a0\u5165\u6c34\u8fdb\u884c\u6d17\u6da4\uff0c\u540c\u65f6\uff0c\u7ee7\u7eed\u52a0\u5165\u4e8c\u6c2f\u7532\u70f7\u8fdb\u884c\u8403\u53d6\u3002\u5408\u5e76\u6709\u673a\u76f8\uff0c\u91c7\u7528\u65e0\u6c34\u786b\u9178\u9541\u8fdb\u884c\u5e72\u71e5\u3002\u51cf\u538b\u9664\u53bb\u6eb6\u5242\u540e\uff0c\u5c06\u7c97\u4ea7\u7269\u901a\u8fc7\u5feb\u901f\u67f1\u8272\u8c31 (\u77f3\u6cb9\u919a\/\u4e59\u9178\u4e59\u916f 2:1 v\/v \u4f5c\u4e3a\u6d17\u8131\u5242)\u5206\u79bb\u7eaf\u5316\u83b7\u5f97\u76f8\u5e94\u03b2-\u5185\u9170\u80fa\u4ea7\u7269\u3002<\/p>\n
\u70ef\u9187\u8d1f\u79bb\u5b50-\u4e9a\u80fa\u73af\u7f29\u5408<\/strong><\/p>\n
0 \u00b0C\u4e0b\uff0c\u5411\u4e8c\u5f02\u4e19\u80fa\u7684\u65e0\u6c34THF\u6eb6\u6db2 (\u6d53\u5ea6\u4e3a0.05 M)\u4e2d\u52a0\u5165\u6b63\u4e01\u57fa\u9502 (2.5 M\u6b63\u5df1\u70f7\u6eb6\u6db2\uff0c\u4e0e\u4e8c\u5f02\u4e19\u80fa\u8ba1\u91cf\u6bd4\u4e3a1:1)\u3002\u7ef4\u63010 \u00b0C\uff0c\u5c06\u4e0a\u8ff0\u5747\u76f8\u6df7\u5408\u7269\u6405\u62cc1 h\uff0c\u4e4b\u540e\u51b7\u5374\u81f3-78 \u00b0C\u3002\u901a\u8fc7\u63d2\u7ba1\u5c06\u916f\u5e95\u7269\u7684\u65e0\u6c34THF\u6eb6\u6db2 (1 eq., \u5e95\u7269\u6d53\u5ea6\u4e3a0.04 M)\u6ef4\u52a0\u81f3\u4e0a\u8ff0\u539f\u4f4d\u751f\u6210\u7684LDA (1.2 eq.)\u4e2d\uff0c\u8d85\u8fc72 h\u540e\uff0c\u6ef4\u52a0\u5b8c\u6bd5\u3002\u968f\u540e\uff0c\u5c06\u4e0a\u8ff0\u6df7\u5408\u7269\u51b7\u5374\u81f3-85 \u00b0C\uff0c\u518d\u5c06\u4e9a\u80fa\u7684\u65e0\u6c34THF\u6eb6\u6db2 (1.3 eq., \u5e95\u7269\u6d53\u5ea6\u4e3a0.05 M)\u6ef4\u52a0\u81f3\u4e0a\u8ff0\u53cd\u5e94\u4f53\u7cfb\u4e2d\uff0c\u8d85\u8fc73 h\u540e\uff0c\u6ef4\u52a0\u5b8c\u6bd5\u3002\u5c06\u4e0a\u8ff0\u53cd\u5e94\u6df7\u5408\u7269\u5347\u81f3\u5ba4\u6e29\uff0c\u6405\u62cc\u76f4\u81f3\u53cd\u5e94\u7ed3\u675f\u3002\u53cd\u5e94\u7ed3\u675f\u540e\uff0c\u52a0\u5165\u9971\u548c\u6c2f\u5316\u94f5\u6eb6\u6db2\u8fdb\u884c\u6dec\u706d\uff0c\u6dec\u706d\u5b8c\u6210\u540e\uff0c\u52a0\u5165\u4e59\u919a\u8fdb\u884c\u8403\u53d6\uff0c\u5c06\u5408\u5e76\u7684\u6709\u673a\u76f8\u91c7\u7528\u65e0\u6c34\u786b\u9178\u9541\u8fdb\u884c\u5e72\u71e5\uff0c\u968f\u540e\uff0c\u51cf\u538b\u9664\u53bb\u6eb6\u5242\u3002\u5c06\u7c97\u4ea7\u7269\u901a\u8fc7\u7845\u80f6\u67f1\u8272\u8c31 (\u6b63\u5df1\u70f7\/\u4e59\u9178\u4e59\u916f 5:1 v\/v \u4f5c\u4e3a\u6d17\u8131\u5242)\u5206\u79bb\u7eaf\u5316\u83b7\u5f97\u76f8\u5e94\u03b2-\u5185\u9170\u80fa\u4ea7\u7269\u3002<\/p>\n
\u672c\u6587\u7248\u6743\u5c5e\u4e8e\u00a0Chem-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 1981\u5e74\u5f00\u59cb\uff0c\u65e5\u672c\u76f8\u6a21\u5316\u5b66\u7814\u7a76\u4e2d\u5fc3 (\u76f8\u6a21\u4e2d\u592e\u5316\u5b66\u7814\u7a76\u6240, Sagami Chemical Research Center)\u7684\u5c3e\u5c9b\u4e25 (\u5c3e\u5cf6 \u5dcc\uff0cOjima Iwao) \u7814\u7a76\u7ec4\u8fdb\u4e00\u6b65\u5c06\u4e0d\u5bf9\u79f0Staudinger\u70ef\u916e-\u4e9a\u80fa[2+2]\u73af\u52a0\u6210 (asymmetric Staudinger ketene-imine [2+2] cycloaddition) [1]-[4]\u53caStaudinger\u4e0d\u5bf9\u79f0\u916f\u70ef\u9187\u8d1f\u79bb\u5b50-\u4e9a\u80fa\u73af\u7f29\u5408 (Staudinger asymmetric ester enolate-imine cyclocondensation) [5]-[7]\u5e94\u7528\u4e8e\u5404\u79cd\u624b\u6027\u03b2-\u5185\u9170\u80fa\u7c7b\u5316\u5408\u7269\u7684\u6784\u5efa[1]-[7]\u3002 \u540c\u65f6\uff0c\u8be5\u8bfe\u9898\u7ec4\u53d1\u73b0\u624b\u6027\u03b2-\u5185\u9170\u80fa\u7c7b\u5316\u5408\u7269\u5728\u5404\u7c7b\u6c28\u57fa\u9178[4], [8]-[12]\u3001\u80bd\u7c7b[13]-[17]\u3001\u975e\u86cb\u767d\u7c7b\u6c28\u57fa\u9178[18]-[19]\u3001taxoid\u6297\u80bf\u7624\u836f[20]-[25]\u3001\u542b\u6c2e\u6742\u73af[26]-[40]\u53ca\u5176\u5b83\u751f\u7269\u6d3b\u6027\u7269\u8d28\u7684\u4e0d\u5bf9\u79f0\u5408\u6210[41]\u4e2d\u5747\u53ef\u4f5c\u4e3a\u5341\u5206\u91cd\u8981\u7684\u5408\u6210\u5b50\u53ca\u5408\u6210\u780c\u5757\uff0c\u56e0\u6b64\uff0c\u6587\u732e\u4e2d\u5c06\u76f8\u5e94\u7684\u624b\u6027\u03b2-\u5185\u9170\u80fa\u79f0\u4e3aOjima\u5185\u9170\u80fa (Ojima lactam)\uff0c\u5c06\u4ee5\u624b\u6027\u03b2-\u5185\u9170\u80fa\u4e3a\u5408\u6210\u5b50\u7684\u65b9\u6cd5\u79f0\u4e3aOjima \u03b2-\u5185\u9170\u80fa\u5408\u6210\u5b50\u65b9\u6cd5 (Ojima \u03b2-lactam synthon method, \u03b2-LSM) [42]\u3002 \u57fa\u672c\u6587\u732e [1] H. Staudinger, Justus Liebigs Ann. Chem. 1907, 356, 51. doi: 10.1002\/jlac.19073560106. [2] I. Ojima, H. J. C. Chen, J. Chem. Soc. Chem. Commun. 1987, 625. doi: 10.1039\/C39870000625. [3] A. K. Bose, M. S. Manhas, J. C. Chib, H. P. S. Chawla, B. Dayal, J. Org. Chem. 1974, 39, 2877. doi: 10.1021\/jo00933a013. [4] N. Hatanaka, I. Ojima, Chem. Lett. 1981, 234. doi: 10.1246\/cl.1981.231. [5] H. Gilman, M. Speeter, J. Am. Chem. Soc. 1943, 65, 2255. […]","protected":false},"author":21,"featured_media":30141,"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":[],"jetpack_publicize_connections":[],"jetpack_featured_media_url":"https:\/\/assets.www.gsbet888.com\/uploads\/2020\/02\/6b61fe61585388f1b6b517dd7310a73e.png","jetpack_shortlink":"https:\/\/wp.me\/p96op1-7PZ","jetpack_sharing_enabled":true,"_links":{"self":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/30131"}],"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=30131"}],"version-history":[{"count":6,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/30131\/revisions"}],"predecessor-version":[{"id":33964,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/posts\/30131\/revisions\/33964"}],"wp:featuredmedia":[{"embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/media\/30141"}],"wp:attachment":[{"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/media?parent=30131"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/categories?post=30131"},{"taxonomy":"post_tag","embeddable":true,"href":"\/\/www.gsbet888.com\/wp-json\/wp\/v2\/tags?post=30131"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}