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張超峰金蟲(chóng) (初入文壇)
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[求助]
求助翻譯一段話(huà),謝謝
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| N-Methylindole was found to react smoothly with iodo-benzene providing an excellent yield (96%) of the C-2 ary-lated product. The reaction also worked well with an electron withdrawing substituent such as nitro on the aryl iodide (entry 2). To check the generality of the procedure the system was extended to various azoles including benzo-thiazole, thiazole, benzoxazole, oxazole and triazole (entries 3–11). Benzothiazole was found to react e ciently with both iodo and the less reactive bromoarene providing good yields of the desired product. Also, electron donating groups such as methyl and methoxy at the ortho or para positions of the iodoarene were viable partners under the present conditions (entries 5, 7, and 10). 1-Methyltriazole was found to be arylated selectively at the more active C-5 position (entry 11). We also tested the applicability of this method with other heteroarenes such as benzothio-phene and benzofuran (entries 12–15). However, reaction of benzothiophene was found to be sluggish using the pre-sent catalytic system, while benzofuran was found to react e ciently with both iodo and bromobenzene providing good yields of the desired product. Encouraged with the above results, the system was further extended to the aryaltion of ca eine, as the products are of interest as adenosine receptor antagonists. Ca eine was arylated e ectively under the present conditions providing an excel-lent yield of 60% of product (entry 16). If C–H activation methodology is not used, the synthetic sequence leading to these compounds requires several steps instead of a single step. |
至尊木蟲(chóng) (著名寫(xiě)手)
| 同時(shí),也研究了鄰、對(duì)位給電子取代基如甲基,甲氧基的影響(entries 5, 7, and 10). 結(jié)果表明,1-甲基三唑選擇性的在高活性的C-5位上發(fā)生芳基化1(entry 11). 我們也檢驗(yàn)了該方法在其他雜環(huán)芳烴如苯并噻吩,苯并呋喃體系中的適用性(entries 12–15). 雖然在現(xiàn)有催化體系中,發(fā)現(xiàn)苯并噻吩的反應(yīng)是很慢的,而苯并呋喃與吲哚以及活性更低的溴代芳烴間都能發(fā)生有效的化學(xué)反應(yīng)并以高產(chǎn)率得到目標(biāo)產(chǎn)物。基于以上實(shí)驗(yàn)結(jié)果,該體系又?jǐn)U展到了ca eine的芳化,因?yàn)樗鼈兊姆磻?yīng)產(chǎn)物可作為有用的腺苷受體拮抗劑。 |
至尊木蟲(chóng) (著名寫(xiě)手)
| 研究發(fā)現(xiàn),N-甲基吲哚可以與碘代苯發(fā)生C-2芳基化反應(yīng),產(chǎn)率高達(dá)96%。該反應(yīng)在帶有強(qiáng)拉電子取代基的芳基吲哚體系中(entry 2). 為了檢驗(yàn)該過(guò)程的普適性,同時(shí)考察了各種唑類(lèi)化合物,包括苯并噻唑,噻唑,苯并惡唑,噁唑以及三唑(entries 3–11). 實(shí)驗(yàn)結(jié)果表明,苯并噻唑與吲哚以及活性更低的溴代芳烴間都能發(fā)生有效的化學(xué)反應(yīng)并以高產(chǎn)率得到目標(biāo)產(chǎn)物。 |
至尊木蟲(chóng) (著名寫(xiě)手)
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