{"id":24165,"date":"2019-01-23T06:15:34","date_gmt":"2019-01-22T22:15:34","guid":{"rendered":"\/\/www.gsbet888.com\/?p=24165"},"modified":"2019-01-23T06:15:34","modified_gmt":"2019-01-22T22:15:34","slug":"angew-chem-int-ed-3%e6%ac%a1%e5%88%86%e5%ad%90%e5%86%85%e5%85%b1%e8%bd%ad%e5%8a%a0%e6%88%90%e5%ae%9e%e7%8e%b0brasilicardin%e7%9a%84%e5%85%a8%e5%90%88%e6%88%90","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/%e5%8c%96%e5%ad%a6%e6%9d%82%e8%ae%b0\/2019\/01\/angew-chem-int-ed-3%e6%ac%a1%e5%88%86%e5%ad%90%e5%86%85%e5%85%b1%e8%bd%ad%e5%8a%a0%e6%88%90%e5%ae%9e%e7%8e%b0brasilicardin%e7%9a%84%e5%85%a8%e5%90%88%e6%88%90.html","title":{"rendered":"Angew. Chem., Int. Ed. 3\u6b21\u5206\u5b50\u5185\u5171\u8f6d\u52a0\u6210\u5b9e\u73b0Brasilicardin\u7684\u5168\u5408\u6210"},"content":{"rendered":"
\u5317\u6d77\u9053\u5927\u5b66\u7684\u8c37\u91ce\u8bfe\u9898\u7ec4\u5b9e\u73b0\u4e86\u5177\u6709\u72ec\u7279\u7a20\u73af\u7ed3\u6784\u7684BrasilicardinA-D\u7684\u7f51\u7f57\u5168\u5408\u6210\u3002\u901a\u8fc7\u4e09\u6b21\u5206\u5b50\u5185\u5171\u8f6d\u52a0\u6210\u5b9e\u73b0\u4e86\u9ad8\u7acb\u4f53\u9009\u62e9\u6027\u7684\u4e09\u7f29\u73af\u5171\u901a\u4e2d\u95f4\u4f53\u662f\u672c\u5168\u5408\u6210\u7684\u5173\u952e\u3002<\/b><\/p>\n Brasilicardin A-D(1<\/b>)<\/span>\u3001\u662f\u4ece\u653e\u5c04\u6027\u75c5\u539f\u83ccNocardia brasiliensis<\/span><\/i>\u7684\u57f9\u517b\u6db2\u4e2d\u5206\u79bb\u3001\u7ed3\u6784\u5df2\u7ecf\u88ab\u786e\u5b9a\u7684\u4e8c\u5e16\u7c7b\u5316\u5408\u7269(\u56fe<\/span>1A)[1]<\/sup><\/span>\u3002Brasilicardin <\/span>A(1a<\/b>)\u5177\u6709\u5f88\u5f3a\u7684\u514d\u75ab\u6291\u5236\u4f5c\u7528\uff0c\u7531\u4e8e\u4f5c\u7528\u673a\u7406\u4e0e\u73b0\u6709\u7684\u514d\u75ab\u6291\u5236\u5242\u4e0d\u540c\uff0c\u56e0\u6b64\u4f5c\u4e3a\u65b0\u578b\u514d\u75ab\u6291\u5236\u5242\u7684lead compound\uff0c\u4e00\u76f4\u53d7\u5230\u9ad8\u5ea6\u5173\u6ce8\u3002 \u4f46\u662f\uff0c\u8ddf\u5929\u7136\u4ea7\u7269\u4e00\u6837\uff0c\u4ece\u81ea\u7136\u4e2d\u83b7\u53d6\u7684\u91cf\u975e\u5e38\u6709\u9650\uff0c\u56e0\u6b64\u5bfc\u81f4\u5176\u836f\u7406\u65b9\u9762\u7684\u7814\u7a76\u5f88\u8fdf\u7f13\u3002\u53e6\u5916\uff0c<\/span>1<\/span><\/b>\u5177\u6709anti-syn-anti\u7a20\u73af<\/span><\/i>\u5168\u6c22\u83f2<\/span>\u9aa8\u67b6(ABC\u73af<\/span>)\uff0c\u53ef\u4ee5\u4e0e\u6c28\u57fa\u9178\u4e0e\u7cd6\u7ed3\u5408\uff0c\u56e0\u6b64\u4e0d\u4ec5\u4ec5\u662f\u751f\u7269\u6d3b\u6027\uff0c\u4ece\u5316\u5b66\u7ed3\u6784\u4e0a\u4e5f\u662f\u975e\u5e38unique\u7684<\/span>\u3002<\/p>\n \u5230\u76ee\u524d\u4e3a\u6b62\u5df2\u7ecf\u62a5\u9053\u4e86\u51e0\u79cd\u90e8\u5206\u5408\u6210\u7684\u5b9e\u4f8b[2]<\/span><\/sup>\u3001\u800c\u5168\u5408\u6210\u4ec5\u4ec5\u53ea\u67092017\u5e74\u7a74\u7530\u8bfe\u9898\u7ec4\u62a5\u9053\u7684\u4e00\u4e2a\u4f8b\u5b50[3]<\/span><\/sup>\u3002\u4ed6\u4eec\u5c06\u4eceWieland-Miescher\u916e\u8f6c\u6362\u7684\u4eb2\u53cc\u70ef\u901a\u8fc7<\/span>Diels-Alder\u53cd\u5e94<\/span><\/a>\u6784\u5efa\u4e86\u590d\u6742\u7684ABC\u73af<\/span>(\u56fe<\/span>1B)<\/span>\u3002\u7136\u540e\uff0c\u5bf9\u4e8e\u5728\u5408\u6210\u7ec8\u76d8\u7684\u7cd6\u57fa\u5316\u90a3\u6b65\uff0c\u7531\u4e8e\u9009\u62e9\u6027\u8131\u4fdd\u62a4\u6bd4\u8f83\u56f0\u96be\u3001\u56e0\u6b64C2\u4f4d\u7684\u7f9f\u57fa\u5728\u65e9\u671f\u5c31\u4e8b\u5148\u5bfc\u5165\uff0c\u6700\u7ec8\u5b9e\u73b01a<\/span><\/b>, 1c<\/b>\u7684\u5168\u5408\u6210\u3002<\/span><\/p>\n \u3000\u8fd9\u6b21\u5317\u6d77\u9053\u5927\u5b66\u7684\u8c37\u91ce\u3001\u5409\u6751\u7b49\u4eba\u3001\u8ba1\u5212\u5728\u5408\u6210\u7ec8\u76d8\u901a\u8fc7\u5bf9\u5171\u901a\u4e2d\u95f4\u4f532<\/span><\/b>\u5b9e\u73b0\u6c28\u57fa\u9178\u7684\u4f4d\u7f6e\uff0c\u5b9e\u73b0\u5bf91<\/strong>\u7684\u7f51\u7f57\u5168\u5408\u6210\u3002\u672c\u5168\u5408\u6210\u7684\u5173\u952e\u4e2d\u95f4\u4f532<\/span><\/b>\u7684ABC\u73af<\/span>\u3001\u4f5c\u8005\u8ba1\u5212\u4ee5\u65b0\u620a\u4e8c\u9187(6<\/b>)\u4e3a\u539f\u6599\u7ecf\u8fc7<\/span>10\u6b65\u5148\u5408\u6210\u5316\u5408\u7269<\/span>5<\/span><\/b>\uff0c\u7136\u540e\u7ecf\u8fc7\u4e09\u6b21\u7acb\u4f53\u9009\u62e9\u6027\u7684\u5206\u5b50\u5185\u5171\u8f6d\u52a0\u6210\u53cd\u5e94\u83b7\u5f97(\u56fe<\/span>1C)<\/span>\u3002<\/p>\n \u56fe1. (A)Brasilicardin A-D (B) \u7a74\u7530\u5408\u6210\u6cd5 (C) \u9006\u5408\u6210\u5206\u6790<\/p>\n<\/div>\n \u201c<\/strong>Asymmetric Total Synthesis of Brasilicardins<\/strong>\u201d<\/strong><\/p>\n Yoshimura, F.; Itoh, R.; Torizuka, M.; Mori, G.; Tanino, K.Angew. Chem., Int. Ed.<\/em>2018<\/strong>,57<\/em>, 17161.<\/p>\n DOI: 10.1002\/anie.201811403<\/a><\/p><\/blockquote>\n \u7814\u7a76\u8005\uff1a\u8c37\u91ce\u572d\u6301<\/a><\/p>\n \u7ecf\u5386\uff1a \u7814\u7a76\u8005\uff1a\u5409\u6751\u6587\u5f66<\/a><\/p>\n \u7ecf\u5386\uff1a \u8bba\u6587\u6982\u8981<\/p>\n \u3000\u4f5c\u8005\u7b49\u4eba\u3001\u8ba1\u5212\u901a\u8fc7\u00a0(1: \u6784\u5efaA, B\u73af<\/span>) \u4e24\u6b21\u5bf9\u03b1,\u03b2-\u4e0d\u9971\u548c<\/span>Weinreb\u9170\u80fa\u7684<\/span>\u03b1-Cyano carbanions\u7684\u5171\u8f6d\u52a0\u6210<\/span>\u3001(2: \u6784\u5efaC\u73af<\/span>) \u5bf9\u03b1,\u03b2-\u4e0d\u9971\u548c\u916f\u7684\u4e59\u70ef\u57fa\u94dc\u7684\u5171\u8f6d\u52a0\u6210\uff0c\u8fd9\u4e24\u4e2a\u5206\u5b50\u5185\u53cd\u5e94\u6765\u6784\u5efaABC\u7a20\u73af<\/span>(\u56fe<\/span>2)<\/span>\u3002<\/p>\n \u5bf9\u4e8e\u53cd\u5e94(1)<\/span>\u3001\u867d\u7136\u4f5c\u8005\u62c5\u5fc3\u8fc7\u5e95\u7269\u7684\u53cd\u5e94\u6027\u4f4e\u3001\u4f46\u662f\u4f7f\u7528NaHMDS\u4f5c\u4e3a\u78b1\u53ef\u4ee5\u5f62\u6210\u7a33\u5b9a\u7684\u9ccc\u5408\u4e2d\u95f4\u4f53<\/span>7<\/span><\/b>\uff0c\u4f7f\u5f97\u53cd\u5e94\u5f88\u9ad8\u6548\u7684\u8fdb\u884c\u3002\u6b64\u5916\uff0c\u5728\u73afA\u7684\u6784\u5efa\u4e2d\uff0c\u901a\u8fc7\u91c7\u8be5\u87af\u5408\u4f5c\u7528\u53ef\u4ee5\u907f\u514d\u4ea7\u751f\u53d1\u751f\u5076\u6781\u6392\u65a5\u7684\u6784\u8c61\uff0c\u4f7f\u5f97\u53cd\u5e94\u5f97\u4ee5\u9ad8\u7acb\u4f53\u9009\u62e9\u6027\u5730\u8fdb\u884c\u3002\u53e6\u4e00\u65b9\u9762\uff0c\u5bf9\u4e8eB\u73af\u7684\u6784\u5efa\uff0c\u901a\u8fc7\u4f7f\u7528\u5177\u6709\u66f4\u5927\u4f4d\u963b\u53d6\u4ee3\u57fa\u53d6\u4ee3\u7684Weinreb\u9170\u80fa<\/span><\/a>\u6765\u63a7\u5236\u751f\u6210\u7269\u7684\u7acb\u4f53\u9009\u62e9\u6027\u3002\u5bf9\u4e8eC\u73af\u7684\u6784\u5efa<\/span>(2)<\/span>\u3001\u4f5c\u8005\u7b49\u4eba\u53c2\u8003\u4e862006\u5e74\u5f00\u53d1\u7684\u4f7f\u7528\u6709\u673a\u94dc\u50ac\u5316\u5242\u5bf91,1-\u4e8c\u6eb4\u70ef\u70c3\u8fdb\u884c\u7684\u73af\u5316\u7684\u65b9\u6cd5[4]<\/span><\/sup>\u3002\u5728\u996d\u5385\u4f53\u7cfb\u4e2d\u4ea7\u751f\u4e59\u70ef\u57fa\u94dc\u4e4b\u540e\u3001\u5347\u6e29\u8fdb\u884c\u4e0e\u03b1,\u03b2-\u4e0d\u9971\u548c\u916f\u7684\u5206\u5b50\u5185\u5171\u8f6d\u52a0\u6210\uff0c\u5f97\u5230\u5168\u5408\u6210\u76ee\u6807\u4ea7\u7269\u4eec\u7684\u5171\u540c\u4e2d\u95f4\u4f53<\/span>2<\/span><\/b>\u3002\u8be6\u7ec6\u53ef\u4ee5\u5177\u4f53\u7ffb\u9605\u8bba\u6587\u3002\u901a\u8fc7\u5bf9\u5171\u540c\u4e2d\u95f4\u4f532<\/span><\/b>\uff0c\u5728\u5408\u6210\u7ec8\u76d8\u8fdb\u884c\u6c28\u57fa\u9178\u90e8\u4f4d\u4e0e\u7cd6\u7684\u4f4d\u7f6e\uff0c\u7acb\u4f53\u9009\u62e9\u6027\u7684\u5bfc\u5165\u6700\u7ec8\u5b9e\u73b0\u4e86Brasilicardin\u00a0<\/span>A-D(1<\/b>)\u7684\u5168\u5408\u6210<\/span>\u3002<\/p>\n \u56fe2. \u5171\u540c\u4e2d\u95f4\u4f533<\/strong>\u7684\u5408\u6210<\/p>\n<\/div>\n \u7efc\u4e0a\u6240\u8ff0\u3001\u4f5c\u8005\u4ece\u5e02\u552e\u7684\u539f\u65996<\/span><\/b>\u51fa\u53d1\u3001\u901a\u8fc737-42\u6b65\u7684\u53cd\u5e94\uff0c\u5b9e\u73b0\u4e86Brasilicardin\u00a0<\/span>A-D\u7684\u5168\u5408\u6210<\/span>\u3002\u5f88\u671f\u5f85\uff0c\u901a\u8fc7\u8fd9\u9879\u5168\u5408\u6210\u7814\u7a76\u53ef\u4ee5\u52a0\u901f\u8be5\u7c7b\u5929\u7136\u4ea7\u7269\u7684\u836f\u7406\u6d3b\u6027\u7684\u7814\u7a76\u3002<\/p>\nBrasilicardin A-D<\/span><\/h4>\n
<\/p>\n
\u8bba\u6587\u4f5c\u8005\u4ecb\u7ecd<\/h4>\n
<\/p>\n
\n1987 \u4e1c\u4eac\u5de5\u4e1a\u5927\u5b66\u5927\u5b66\u9662\u7406\u5de5\u5b66\u7814\u7a76\u79d1\u5316\u5b66\u4e13\u4e1a\u7855\u58eb\u5b66\u4f4d(\u6851\u5cf6\u529f\u6559\u6388)
\n1989 \u4e1c\u4eac\u5de5\u4e1a\u5927\u5b66\u5927\u5b66\u9662\u7406\u5de5\u5b66\u7814\u7a76\u79d1\u5316\u5b66\u4e13\u4e1a\u535a\u58eb\u4e2d\u9000
\n1989 \u4e1c\u4eac\u5de5\u4e1a\u5927\u5b66\u7406\u5b66\u90e8\u5316\u5b66\u79d1\u52a9\u624b
\n1994 \u4e1c\u4eac\u5de5\u4e1a\u5927\u5b66\u535a\u58eb\u5b66\u4f4d\uff08\u7406\u5b66\uff09
\n1998 \u5317\u6d77\u9053\u5927\u5b66\u5927\u5b66\u9662\u7406\u5b66\u9662\u5316\u5b66\u4e13\u4e1a\u52a9\u624b
\n1999 \u5317\u6d77\u9053\u5927\u5b66\u5927\u5b66\u9662\u7406\u5b66\u7814\u7a76\u79d1\u5316\u5b66\u4e13\u4e1a\u52a9\u7406\u6559\u6388
\n2006- \u5317\u6d77\u9053\u5927\u5b66\u5927\u5b66\u9662\u7406\u5b66\u7814\u7a76\u9662\u5316\u5b66\u90e8\u95e8\u6559\u6388
\n\u7814\u7a76\u5185\u5bb9\uff1a\u6709\u673a\u91d1\u5c5e\u6216\u8005\u8fc7\u6e21\u91d1\u5c5e\u50ac\u5316\u7684\u65b0\u53cd\u5e94\u5f00\u53d1\u3001\u5929\u7136\u4ea7\u7269\u5168\u5408\u6210<\/p>\n<\/p>\n
\n2002 \u4e1c\u5317\u5927\u5b66\u5927\u5b66\u9662\u7406\u5b66\u7814\u7a76\u79d1\u535a\u58eb\u5b66\u4f4d(\u5e73\u9593\u6b63\u535a\u6559\u6388)
\n2002 \u7f8e\u56fd\u65af\u9686-\u51ef\u7279\u7433\u7814\u7a76\u6240\u535a\u58eb\u540e
\n2004 \u5317\u6d77\u9053\u5927\u5b66\u5927\u5b66\u9662\u7406\u5b66\u7814\u7a76\u79d1\u52a9\u624b
\n2007 \u5317\u6d77\u9053\u5927\u5b66\u5927\u5b66\u9662\u7406\u5b66\u7814\u7a76\u9662\u52a9\u7406\u6559\u6388
\n2017- \u9759\u5188\u53bf\u7acb\u5927\u5b66\u836f\u5b66\u90e8\u526f\u6559\u6388
\n\u7814\u7a76\u5185\u5bb9\uff1a\u590d\u6742\u7ed3\u6784\u7684\u751f\u7269\u6d3b\u6027\u5929\u7136\u4ea7\u7269\u5168\u5408\u6210\u3001\u65b0\u53cd\u5e94\u7684\u5f00\u53d1<\/p>\n<\/p>\n
\u53c2\u8003\u6587\u732e<\/h4>\n
\n