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A practical synthesis of trifluorophenyl R-amino acid:The key precursor for the new anti-diabetic drug sitagliptin

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Chinese Chemical Letters 2009年第12期20卷 1397-1399页

作者： Li Li Zeng ying Jie ding Gui Cheng Zhang Hong Rui Song Wen Hui Hu Laboratory of Anti-diabetic Drug Discovery Center for Synthetic and Natural Drugs Guangzhou Institute of Biomedicine and Health Chinese Academy of Sciences Guangzhou 510663 China The School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 China

Sitagliptin is the first new anti-diabetic drug in DPP-Ⅳ inhibitor class. The general synthesis of sitagliptin is by coupling of the β-amino acid fragment with the heterocycle fragment. Though the specific β-amino acid can be easily made from the corresponding R-amino acid by Arndt-Eistert hornologation, the optically pure precursor R-amino acid is difficult to prepare. We herein reported a practical protocol to make the trifluorophenyl substituted R-amino acid 4 in 〉99.9% ee and 40.3% yield by the enzymatic resolution employing enantioselective hydrolysis and a general separation procedure. This protocol requires only cheap starting materials and friendly reaction condition. The procedure not only allows people to prepare the drug substance, but also provides an alternative method for prepareing the rare α-amino acid and the subsequent β-amino acid.

关键词： Sitagliptin β-Amino acid DPP-Ⅳ inhibitor Practical synthesis

Usefulness of two-point Dixon fat-water separation technique in gadoxetic acid-enhanced liver magnetic resonance imaging

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World Journal of Gastroenterology 2015年第16期21卷 5017-5022页

作者： ying ding Sheng-Xiang Rao Cai-Zhong Chen Ren-Chen Li Meng-Su Zeng Department of Radiology Zhongshan Hospital of Fudan UniversityShanghai Institute of Medical Imaging

AIM:To compare differences between volumetric interpolated breath-hold examination(VIBE) using two-point Dixon fat-water separation(Dixon-VIBE) and chemically selective fat saturation(FS-VIBE) with magnetic resonance imaging ***:Forty-nine patients were included, who were scanned with two VIBE sequences(Dixon-VIBE and FS-VIBE) in hepatobiliary phase after gadoxetic acid *** evaluations including sharpness of tumor, sharpness of vessels, strength and homogeneity of fat suppression, and artifacts that were scored using a 4-point *** liver-to-lesion contrast was also calculated and ***:Dixon-VIBE with water reconstruction had significantly higher subjective scores than FS-VIBE in strength and homogeneity of fat suppression(< 0.0001) but lower scores in sharpness of tumor(P < 0.0001), sharpness of vessels(P = 0.0001), and artifacts(P = 0.034).The liver-to-lesion contrast on Dixon-VIBE images was significantly lower than that on FS-VIBE(16.6% ± 9.4% vs 23.9% ± 12.1%, P = 0.0001).CONCLUSION:Dixon-VIBE provides stronger and more homogenous fat suppression than FS-VIBE, while has lower clarity of focal liver lesions in hepatobiliary phase after gadoxetic acid administration.

关键词： Dixon-volumetric interpolated breath-holdexamination Fat saturation-volumetric interpolatedbreath-hold examination Gadoxetic acid Volumetricinterpolated breath-hold examination Magnetic resonance imaging

REALIZING ChINESEAND RUSSIAN DREAMS

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Beijing Review 2013年第13期56卷 12-17页

作者： ding ying

Everyone＇s dream is different. But most countries＇ are similar, to make themselves strong and prosperous. For two neighboring powers like China and Russia, promoting bilateral cooperation is helpful in turning such dreams into reality, due to a common interest in development and responsibility in maintaining peace and stability in the neighborhood, as well as the world.

关键词：中国经济建设经济发展民生问题

PROSPEROUS XINJIANG Rapid development brings harmony and prosperity to China’s vast western region

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Beijing Review 2011年第32期54卷 16-21页

作者： ding ying

In China,most people are familiar with a song created in the early 1950s saying:Our Xinjiang is a beautiful *** pastures on both sides of the Tianshan Mountains… Today Xinjiang Uygur Autonomous Region in northwest Ch...

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OUT OF LIBYA

Beijing Review 2011年第10期54卷 10-15页

作者： ding ying

China completes a historic evacuation of 35,860 Chinese citizens from Libya within days February 18 was a bad day for 37-year-old Deng *** night, a group of Libyan looters raided the Chinese hydro-power

关键词： OUT OF LIBYA

Analysis of the Cellular Localization of Herpes Simplex Virus 1 Immediate-early Protein ICP22

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Virologica Sinica 2010年第3期25卷 158-167页

作者： Wei CUN Jie CHEN ying ZHANG Long-ding LIU Qi-han LI Institute of Medical Biology Chinese Academy of Medical Sciences Peking Union Medical College Kunming 650118 China

Nuclear proteins often form punctiform structures, but the precise mechanism for this process is unknown. As a preliminary study, we investigated the aggregation of an HSV-1 immediate-early protein, infected-cell protein 22 （ICP22）, in the nucleus by observing the localization of ICP22-EGFP fusion protein Results showed that, in high-level expression conditions, ICP22-EGFP gradually concentrates in the nucleus, persists throughout the cell cycle without disaggregation even in the cell division phase, and is finally distributed to daughter cells. We subsequently constructed a mammalian cell expression system, which had tetracycline- dependent transcriptional regulators. Consequently, the location of ICP22-EGFP in the nucleus changed with distinct induction conditions. This suggests that the cellular location of ICP22 is also influenced by promoter regulation, in addition to its own structure. Our findings provide new clues for the investigation of transcriptional regulation of viral genes. In addition, the non-protease reporter system we constructed could be utilized to evaluate the role of intemal ribosome entry sites （IRES） on transcriptional regulation.

关键词： Herpes Simplex Virus 1 (HSV-1) ICP22 Transcriptional regulation Cellular localization Nuclear functional domain

Prescription for Poverty Reduction

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Beijing Review 2020年第44期63卷 32-33页

作者： ding ying 不详

The novel coronavirus disease(COVID-19)has not monly afferter the economies of countries and regions but also poses a challenge to the United Nations Sustainable Dewelopment Goal (SDG) of ending poverty by 2030.

关键词： Sustainable Poverty poverty

Continued Calls for Peace

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Beijing Review 2012年第45期55卷 26-27页

作者： ding ying

China continues to fight for its sov- ereignty and territorial integrity through words and actions. The country＇s marine surveillance fleet has expelled a number of Japmlese vessels sailing illegally in waters around... 详细信息

关键词：东中国海海洋监视近海域钓鱼岛

For a Safer And Better World

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Beijing Review 2022年第21期65卷 22-25页

作者： ding ying 不详

What does an ideal world look like?For many around the globe,the answer is quite simple:A much more friendly,helping environment compared to today’s *** the peaceloving civilization,the Chinese *** 2,500 years ago,amid the chaos stemming from successive wars between vassal states,the philosopher and politician Confucius (551-479 B.C.) proposed a type of"great harmony"in which people live in peace and help each other grow。

关键词： harmony peace quite