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暮霭沉沉楚新虫 (初入文坛)
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[求助]
求大神翻译一段英文文献
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(±)-β-(3,4-Dihydroxyphenyl) lactic acid ((±)-DSS) and its derivatives have recently attracted considerable interest due to their potential pharmaceutical activities for anti-oxidation,1 anticoagulance, 2 anti-myocardial ischemia,3 anti-inflammation,4 and anti-neoplasticism.5 Our previous studies6 on distribution and metabolites of Danshen (Salvia miltiorrhiza bunge) and Danshen dripping pills (a patented traditional Chinese medicine consisting of radix salvia miltiorrhizae, radix notoginseng, and borneolum syntheticum) with rabbits suggested that compounds 2 and 3 (Figure 1) might play a key role in the patent medicine of Danshen. Along with studies on the correlation of (±)-DSS, (±)-IDHP, and (±)-DBZ in vivo and their pharmacokinetics and pharmacodynamics, a considerable number of methods to synthesize substituted (±)-DSS and their key intermediates7 have been investigated. For example, we developed a synthesis process (Scheme 1),8 which was based on a previously published strategy;9,12 the process involved five steps resulting in an overall yield of only 12%. To improve its yield and avoid using toxic mercury catalysts, an alternative route10 was utilized. However, its overall yield of 18% was also not satisfied for large-scale production. In addition, asymmetric synthesis of IDHP and DBZ was developed by our group,11 but its high cost made it economically not viable for large-scale production. Therefore, there still remain challenges for the production of these derivatives in quality and quantity sufficient for pharmaceutical applications. The aim of the present studies was to develop a pilot-scale synthetic method which can deliver higher yields for the (±)-DSS, (±)-IDHP, and (±)-DBZ production. The use of less toxic catalysts was also investigated for a greener process. Furthermore, we developed a method for chiral separation of (±)-IDHP and (±)-DBZ to give an optical purity (>99% ee) isomer of R-IDHP, S-IDHP, R-DBZ, and S-DBZ. |
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金虫 (正式写手)
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暮霭沉沉楚: 金币+20, ★有帮助, 我想知道就是你翻不出来的那几个词！！不过还是谢谢了 2015-12-16 00:07:46
暮霭沉沉楚: 金币+20, ★有帮助, 我想知道就是你翻不出来的那几个词！！不过还是谢谢了 2015-12-16 00:07:46
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乳酸(±)-β-(3,4-Dihydroxyphenyl)及其衍生物凭借潜在的抗氧化性、抗凝血性、抗心肌梗缺氧、抗炎症及抗肿瘤功能等医药作用已经得到广泛关注。我们之前用小白鼠研究了丹参和丹参滴丸的分布及代谢产物，结果显示复合物2和3可能在中成药丹参里发挥着重要作用。同时，我们还研究了(±)-DSS、(±)-IDHP和(±)-DBZ在活体内的相关性，合成取代(±)-DSS的大量方法以及关键的中间体。例如，我们基于之前已报道的理论开发了一种合成方法8，该方法包括5步，而总产率仅百分之十二。为了提高产率并避免使用有毒的汞催化剂，我们使用了可替代的合成路线10,然而其总产率为百分之十八，仍不能满足大规模的生产。此外，我们也开发了IDHP和DBZ的非对称合成法，但是其高成本导致该方法在大规模生产中经济上不可行。因此开发保质保量的合成方法已满足制药行业的应用仍存在很多挑战。 目前的研究目标是开发一种能中试规模的合成方法，已提高(±)-DSS, (±)-IDHP, and (±)-DBZ的生产率，同时，为绿色合成过程寻找毒性更小的催化剂。而且，我们也为(±)-IDHP 和 (±)-DBZ的手性拆分开发了一种方法，从而得到光学纯度的 R-IDHP, S-IDHP, R-DBZ, 和 S-DBZ的同分异构体。 外行 仅供参考 有些专业词汇楼主自己查一下吧 |
2楼2015-12-15 23:55:54
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