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暮靄沉沉楚

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[求助] 求大神翻譯一段英文文獻(xiàn)

(±)-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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1樓 2015-12-14 19:55:24

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【答案】應(yīng)助回帖

★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★
暮靄沉沉楚: 金幣+20, ★有幫助, 我想知道就是你翻不出來的那幾個(gè)詞！！不過還是謝謝了 2015-12-16 00:07:46

乳酸(±)-β-(3,4-Dihydroxyphenyl)及其衍生物憑借潛在的抗氧化性、抗凝血性、抗心肌梗缺氧、抗炎癥及抗腫瘤功能等醫(yī)藥作用已經(jīng)得到廣泛關(guān)注。我們之前用小白鼠研究了丹參和丹參滴丸的分布及代謝產(chǎn)物，結(jié)果顯示復(fù)合物2和3可能在中成藥丹參里發(fā)揮著重要作用。同時(shí)，我們還研究了(±)-DSS、(±)-IDHP和(±)-DBZ在活體內(nèi)的相關(guān)性，合成取代(±)-DSS的大量方法以及關(guān)鍵的中間體。例如，我們基于之前已報(bào)道的理論開發(fā)了一種合成方法8，該方法包括5步，而總產(chǎn)率僅百分之十二。為了提高產(chǎn)率并避免使用有毒的汞催化劑，我們使用了可替代的合成路線10,然而其總產(chǎn)率為百分之十八，仍不能滿足大規(guī)模的生產(chǎn)。此外，我們也開發(fā)了IDHP和DBZ的非對(duì)稱合成法，但是其高成本導(dǎo)致該方法在大規(guī)模生產(chǎn)中經(jīng)濟(jì)上不可行。因此開發(fā)保質(zhì)保量的合成方法已滿足制藥行業(yè)的應(yīng)用仍存在很多挑戰(zhàn)。
目前的研究目標(biāo)是開發(fā)一種能中試規(guī)模的合成方法，已提高(±)-DSS, (±)-IDHP, and (±)-DBZ的生產(chǎn)率，同時(shí)，為綠色合成過程尋找毒性更小的催化劑。而且，我們也為(±)-IDHP 和 (±)-DBZ的手性拆分開發(fā)了一種方法，從而得到光學(xué)純度的 R-IDHP, S-IDHP, R-DBZ, 和 S-DBZ的同分異構(gòu)體。
外行僅供參考有些專業(yè)詞匯樓主自己查一下吧

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2樓2015-12-15 23:55:54