施小新-全讯国际

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施小新 (xiao-xin shi)  教授 博士生导师
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电话: 02164252052
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个人简介
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  1985年本科毕业于苏州大学化学系;1991年于中国科学院上海有机化学研究所获得理学博士学位;1991-1993年期间在中国科学院上海有机化学研究所工作,任助理研究员;1993-1996年期间在美国佛罗里达工学院(fit,florida institute of technology)健康与治疗研究中心进行博士后研究工作;1996-2000年期间,回中国科学院上海有机化学研究所工作,任副研究员,2000-2001年期间,在华东理工大学工作,任副教授;2001年至今,继续在华东理工大学工作,任教授;2003年起,为博士生导师。
 

研究方向
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  不对称合成和合成药物化学。
 

获奖成果
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  参加并获得2002年度上海市科技进步一等奖和2003年度国家自然科学二等奖。
2003年度上海市教委的曙光计划。
 

代表性论著
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1, jin-yu lai, xiao-xin shi and li-xin dai*,“reversal of regiochemistry of wacker-type reactions oriented by heteroatoms”, j. org. chem., 1992, 57, 3485.

2, xiao-xin shi and li-xin dai*, “halogenation of stablized ester enolates by cupric halides”, j. org. chem., 1993, 58, 4596.

3, jin-yu lai, xiao-xin shi, yan-shen gong and li-xin dai*, “palladium-catalyzed synthesis of optically active tetrahydro-1,4-oxazine derivatives”, j. org. chem., 1993, 58, 4775.

4, steven s. wang, xiao-xin shi, william s. powell, tamara tieman, steven j. feinmark and joshua rokach*, “total syntheses of proinflammatory dihydro-12-kete metabolites”, tetrahedron lett., 1995, 36, 513.

5, xiao-xin shi, subhash p. khanapure and joshua rokach*, “deblocking of dithioacetals and oxathioacetals using periodic acid under mild nonaqueous conditions”, tetrahedron lett., 1996, 37, 4331.

6, subhash p. khanapure, xiao-xin shi, william s. powell and joshua rokach*, “total syntheses of a potent proinflammatory 5-oxo-ete and its 6,7-dihydro biotransformation product”, j. org. chem., 1998, 63, 337.

7, subhash p. khanapure, xiao-xin shi, william s. powell and joshua rokach*, “total syntheses of tritiated and deuterated 5-oxo-ete, a novel inflammatory mediator”, j. org. chem., 1998, 63, 4098.

8, xiao-xin shi* and qing-quan wu, “deblocking of dithianes with diacetoxyiodobenzene”, syn. commun., 2000, 30, 4081.

9, xiao-xin shi*, qing-quan wu and xia lu, “a synthesis of (4s)-2-(acetoxymethyl)- 4-(tert-butyl-diphenylsilyloxy)-2-cycpenten-1-one”, tetrahedron:asymmetry, 2002, 13, 461-464.

10, xiao-xin shi*, wei he, qing-quan wu, jie yin, feng ni and xiao-zhou jin, “asymmetric synthesis of (1s,6r,7s,9r)-7,9-bis(tert-butyldiphenylsilyloxy)- 3-oxabicyclo[4,3,0]nonan-2-one”, tetrahedron:asymmetry, 2004, 15, 2327-2331.

11, xiao-xin shi*, jian-zhong yao, li kang, chun-li shen and fei yi, “asymmetric syntheses of both enantiomers of amphetamine hydrochloride via bakers’ yeast reduction of phenylacetone”, j. chem. res., 2004, 10, 681.

12, zhao-xia wang, xiao-xin shi, guo-rong chen*, zhi-hua ren, lei luo and jing yan, “a new synthesis of α-arbutin via lewis acid catalyzed selective glycosylation of tetra-o-benzyl-α-d-glucopyranosyl trichloroacetimidate with hydroquinone”, carbohydrate res., 2006, 341, 1945-1947.

13, minze zhu, chuantao cha, wei-ping deng* and xiao-xin shi*, “a mild and efficient catalyst for the beckmann rearrangement, bop-cl”, tetrahedron lett., 2006, 47, 4861-4863.

14, xiao-xin shi*, feng ni, hai-xia shang, ming-le yan and jun-quan su, “racemization of (s)-( )-10,11-dimethoxyaporphine and (s)-( )-aporphine: efficient preparations of (r)-(-)-apomorphine and (r)-(-)-aporphine via a recycle process of resolution”, tetrahedron:asymmetry, 2006, 17, 2210-2215.

15, xiao-xin shi*, shi-ling liu, wei xu, and yu-lan xu, "highly stereoselective pictet-spengler reaction of d-tryptophan methyl ester with piperonal: convenient syntheses of cialis (tadalafil), 12a-epi-cialis and their deuterated analogues", tetrahedron: asymmetry, 2008, 19, 435-442.

16, liang-deng nie, xiao-xin shi*, "a novel asymmetric synthesis of oseltamivir phosphate (tamiflu) from (-)-shikimic acid", tetrahedron: asymmetry, 2009, 20, 124-129.

17,  shi-ling liu, xiao-xin shi,* yu-lan xu, wei xu, jing dong,  "asymmetric syntheses of (-)-methyl shikimate and (-)-5a-carba-β-d-gulopyranose from d-arabinose via mukaiyama-type intramolecular aldolization", tetrahedron: asymmetry, 2009, 20, 78-83.

18, sen xiao, xia lu, xiao-xin shi*, yu sun, li-li liang, xin-hong yu and jing dong, "syntheses of chiral 1,3-disubstituted tetrahydro-β-carbolines via ciat process: highly stereoselective pictet-spengler reaction of d-tryptophan ester hydrochlorides with various aldehydes", tetrahedron: asymmetry, 2009, 20, 430-439.

19, liang-deng nie, xiao-xin shi*, kwang hyok ko and wei-dong lu, "a short and practical synthesis of oseltamivir phosphate (tamiflu) from (-)-shikimic acid", j. org. chem. 2009, 74, 3970-3973.

20,  sen xiao, xiao-xin shi*, jing xing, jing-jing yan, shi-ling liu and wei-dong lu, "synthesis of tadalafil (cialis) from l-tryptophane", tetrahedron: asymmetry, 2009, 20, 2090-2096.

21, sen xiao, xiao-xin shi*, feng ni, jing xing, jing-jing yan, and shi-ling liu, "an efficient and general method for the stereodivergent syntheses of tadalafil-like tetracyclic compounds", eur. j. org. chem., 2010, 1711-1716.

22, xiao-xin shi*, chun-li shen, jian-zhong yao, liang-deng nie, and na quan, "inversion of secondary chiral alcohols in toluene with the tunable complex of r3n-r'cooh", tetrahedron: asymmetry, 2010, 21, 277-284.

23, sen xiao, and xiao-xin shi*, "the first highly stereoselective approach to the mitotic kinesin eg5 inhibitor hr22c16 and its analogues", tetrahedron: asymmetry, 2010, 21, 226-231.

24,jing dong, xiao-xin shi*, jing-jing yan, jing xing, qiang zhang, and sen xiao, “efficient and practical one-pot conversions of n-tosyl tetrahydroisoquinolines into isoquinolines and n-tosyl tetrahydro-β-carbolines into β-carbolines via tandem β-elimination and aromatization”, eur. j. org. chem.2010, 6987-6992.

25, na quan, xiao-xin shi*, liang-deng nie, jing dong, rui-heng zhu, “a green chemistry method for the regeneration of carbonyl compounds from oximes by using cupric chloride dihydrate as a recoverable promoter for hydrolysis”, synlett 2011, 1028-1032.

26, rui-heng zhu, xiao-xin shi*, “practical and highly stereoselective method for the preparation of several chiral arylsulfinamides and arylsulfinates based on spontaneous crystallization of diastereomerically pure n-benzyl-n-(1-phenylethyl) -arylsulfinamides”, tetrahedron: asymmetry 2011, 22, 387-393.

27, xiao-peng he, zhuo song, zhi-zhou wang, xiao-xin shi*, kaixian chen*, guo-rong chen*, “creation of 3,4-bis-triazolocoumarian-sugar conjugates via flourogenic dual click chemistry and their quenching specificity with silver(i) in aqueous media”, tetrahedron 2011, 67, 3343-3347.

28, jing dong, tien ha trieu, xiao-xin shi*, qiang zhang, sen xiao, xia lu, “a general strategy for the highly stereoselective synthesis of hr22c16-like mitotic kinesin eg5 inhibitors from both l- and d-tryptophans”, tetrahedron: asymmetry 2011, 22, 1865-1873.

29, liang-deng nie, xiao-xin shi*, na quan, fei-feng wang, xia lu, “novel asymmetric synthesis of oseltamivir phosphate (tamiflu) from (-)-shikimic acid via cyclic sulfite intermediates”, tetrahedron: asymmetry 2011, 22, 1692-1699.

30, rui-heng zhu, xiao-xin shi*, “synthesis of diaryl disulfides via mild reduction of arylsulfinates with hydrazine monohydrate in dmso”, synth. commun. 2012, 42, 1108-1114.

31, jing dong, xiao-xin shi*, jing xing, jing-jing yan, “mild and efficient syntheses of 1-aryl-3,4-dihydroisoquinolines and 1-aryl-3,4-dihydro-β-carbolines via regiospecific β-eliminations of the corresponding n-tosyl-1,2,3,4-tetrahydro isoquinolines and n-tosyl-1,2,3,4-tetrahydro-β-carbolines”, synth. commun. 2012, 42, 2806-2817. 

32qiang zhang, jing dong, xiao-xin shi*, xia lu,total syntheses of dichotomines a–d and the stereochemical revision of dichotomines b–d”. eur. j. org. chem. 2012, 3317-3325. 

33liang-deng nie, wei ding, xiao-xin shi*, na quan, xia lu, “a novel and high-yielding asymmetric synthesis of oseltamivir phosphate (tamiflu) starting from (-)-shikimic acid”. tetrahedron: asymmetry 2012, 23, 742-747. 

34, na quan, liangdeng nie, xiaoxin shi*, ruiheng zhu, xia lu, “novel and efficient syntheses of four useful shikimate-derived epoxy chiral building blocks via cyclic sulfite intermediates”, chin. j. chem. 2012, 30, 2759-2766. 

 

35. jianxin yang, jing dong, xia lu, qiang, zhang, wei ding, xiaoxin shi*, “ethylenediamine: a highly effective catalyst for one-pot synthesis of aryl nitroalkenes via henry reaction and dehydration”, chin. j. chem. 2012, 30, 2827-2833.  

36. qiang zhang, zhen fan, jing dong, xiao-xin shi*, xia lu, “novel asymmetric total syntheses of (r)-(-)-pyridindolol, (r)-(-)-pyridindolol k1, and (r)-(-)-pyridindolol k2 via a mild one-pot aromatization of n-tosyl-tetrahydro-β- carboline with (s)-2,3- o-isopropylidene-l-glyceraldehyde as the source of chirality”, tetrahedron: asymmetry2013, 24, 633–637.

37. liang-deng nie, fei-feng wang, wei ding, xiao-xin shi*, xia lu, “a novel azide-free asymmetric synthesis of oseltamivir phosphate (tamiflu) starting from roche’s epoxide”, tetrahedron: asymmetry2013, 24, 638–642.

38. tien ha trieu, jing dong, qiang zhang, bo zheng, tian-zhuo meng, xia lu, and xiao-xin shi*, “total syntheses of eudistomins y1–y7 via an efficient one-pot process of tandem benzylic oxidation and aromatization of1-benzyl-3,4-dihydro-β-carbolines.” eur. j. org. chem. 2013, 3271–3277

39. na quan, liang-deng nie, rui-heng zhu, xiao-xin shi*, wei ding, and xia lu, “total syntheses of ( )-valiolamine and (–)-1-epi-valiolamine from naturally abundant (–)-shikimic acid”, eur. j. org. chem. 2013, 6389–6396.

 
40. jing dong, tian-zhuo meng, xiao-xin shi*, wen-hui zou, xia lu, “highly stereoselective transformation of (1s,3s)-cis-1,3-disubstituted tetrahydro-b-carbolines into (1s,3r)-trans-1,3-disubstituted tetrahydro-b-carbolines: an improved asymmetric synthesis of tadalafil from l-tryptophan”, tetrahedron: asymmetry 2013, 24, 883–893. 

41. tien ha trieu, jing dong, xiao-xin shi*, xia lu, and qiang zhang, “efficient and benign one-pot conversion of n-tosyl-1,4,5,6-tetrahydropyrimidines to pyrimidines via tandem β-elimination and aromatization”, synthetic communications, 2013, 43, 3141-3152.

 

译著:1,《当代新药合成》,施小新、秦川译,荣国斌校.2005年华东理工大学出版社出版。
2,《工业不对称催化》, 施小新、冀亚飞、邓卫平译,邓卫平校.华东理工出版社,2006年。
 
 

 

 

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