2-(1-Bromoethyl)Naphthalene置于氢氧化钾体系中,用 乙醇,溶剂黄146 作为反应溶剂,化学反应生成 1-(2-萘甲酰基)乙醇 参考文献:Synthetic Studies On Anthracyclinones. Xiii. Conversion Of Bisanhydro-γ-Rhodomycinone Into Bisanhydrodaunomycinone 标题:Synthetic Studies On Anthracyclinones. Xiii. Conversion Of Bisanhydro-γ-Rhodomycinone Into Bisanhydrodaunomycinone 摘要:如图 2 所示,通过 7 个步骤,将 Iii 中的乙基侧链转化为乙酰基,从而通过双脱水-γ-罗多霉素酮(iii)合成了双脱水-γ-罗多霉素酮(II).通过红外光谱和紫外光谱的比较,讨论了 6,11-二羟基萘醌(ii 和 Iii)甲基化过程中形成的厌醌体系. DOI:10.1248/cpb.22.93
专利号:US-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
专利号:US-2004014168-A1 优先权日:1998-06-11 标题:Reagents and methods for library synthesis and screening 发明人:SCHREIBER STUART L; BLACKWELL HELEN E; PEREZ FERNANDEZ LUCY; TALLARICO JOHN A 权利人:HUGHES HOWARD MED INST 摘要:The invention provides novel solid supports for the synthesis of compound libraries. The solid supports have the physical capacity to deliver at least 50 nmol of compound and are functionalized with a silicon-containing linker. In one embodiment of the invention the solid support comprises a bead having a diameter of between approximately 400 and 600 μm functionalized with a silicon-containing linker. According to certain embodiments of the invention the bead is a polystyrene bead. According to certain embodiments of the invention the linker is a diisopropylalkyl-substituted silyl ether. The invention further provides grafted polymeric supports such as lanterns functionalized with a silicon-containing linker. n The invention provides methods for screening in which compounds are synthesized on solid supports in a quantity so that a single solid support such as a bead provides a stock solution sufficient to perform hundreds or thousands of biological or chemical assays. The methods include decoding the sequence of chemical reactions used to synthesize the compound by identifying tags incorporated into the compound during synthesis.
专利号:US-8138272-B2 优先权日:2006-05-22 标 题:Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds 发明人:KONRADI ANDREI W; SMITH JENIFER L 权利人:KONRADI ANDREI W; SMITH JENIFER L; ELAN PHARM INC 摘要:This invention provides an improved synthesis of polymer conjugates of formula (I), n nof agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treating primary or secondary alcohol substituents of active compounds with polymeric nucleophiles using “Mitsunobuâ€? or related reaction conditions.
专利号:US-7763734-B2 优先权日:2006-04-19 标题 :Synthesis, structure and use of bisoxazolidines for asymmetric catalysis and synthesis 发明人:WOLF CHRISTIAN; LIU SHUANGLONG 权利人:UNIV GEORGETOWN 摘要:One aspect of the invention relates to chiral bisoxazolidines and their use in asymmetric catalysis. The chiral bisoxazolidines are a novel class of compounds that is expected to find multiple applications, for example, in asymmetric synthesis. For example, a bisoxazolidine ligand enabled the catalytic enantioselective alkynylation and alkylation of a range of aromatic and aliphatic aldehydes, generating chiral propargylic alcohols and secondary alcohols in high yields and enantiomeric excess.
专利号:US-7750135-B2 优先权日:2006-07-28 标题:Molecular design of thermostable alcohol dehydrogenase for synthesis for chiral aromatic alcohols 发明人:ZEIKUS J GREGORY; ZIEGELMANN-FJELD KARLA I; VIEILLE CLAIRE 权利人:UNIV MICHIGAN STATE 摘要:The present invention relates to compositions and methods utilizing thermostable and novel alcohol dehydrogenase enzymes for biosynthesizing chiral specific molecules for use as precursor molecules in synthesizing pharmaceutical compounds. Particularly, in preferred embodiments, the invention relates to directed engineering of an enzymatic catalytic site of an alcohol dehydrogenase enzyme gene for enhancing enantioselectivity for (S)-enantiomer substrate catalytic activity for providing aryl (S)-enantiomer products in stereomeric excess.
专利号:US-5075339-A 优先权日:1989-07-28 标 题:Benzylketone phospholipase A2 inhibitors 发明人:WILKERSON WENDELL W 权利人:DU PONT MERCK PHARMA 摘要:The invention relates to benzylketone phospholipase A2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A2-mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylketone phospholipase A2 inhibitor. These compounds are also intermediates in the synthesis of other PLA2 inhibitors.
[参考文献]: K Le Barbu-Debus, Et Al. Chiral Recognition In Jet-Cooled Complexes Of (1R,2S)-(+)-Cis-1-Amino-2-Indanol And Methyl Lactate: On The Importance Of The Ch...Pi Interaction. Phys Chem Chem Phys. 2009 Sep 21;11(35):7589-98.
合成参考文献
参考文献:10.1107/s1600536811015820 摘要:Solak S, Karakuş M, Tercan B, Hökelek T. Triethyl-ammonium (S)-(-)-O-[1-(2-naphth-yl)eth-yl] (4-meth-oxy-phen-yl)dithio-phospho-nate. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1260–1.