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1.  An improved synthesis of(lS,4S)-2-oxa-5-azabicyclo[2.2.1]heptane  
   Dong-Feng Zhang  Peng Li  Zi-Yun Lin  Hai-Hong Huang《中国化学快报》,2014年第25卷第3期
   An improved and efficient method for synthesis of(lS,4S)-2-oxa-5-azabicyclo[2.2.1]heptane(1) from trans-4-hydroxy-L-proline was developed. Using benzyloxycarbonyl(Cbz) as protection group of amine, the reactions were inmild conditions, and the title compound 1 was accomplished in six steps in overall yield of 70%.    

2.  Synthesis and Characterization of Aryl Acylguanidines and Their Copper(Ⅱ) Complexes  
   周启  张志娇  王凡凡  韩立  朱成奔  李海普  杨鹰《结构化学》,2019年第8期
   A series of eight N-mono-substituted aryl acylguanidines L~(1~8) were synthesized from the reactions of their parent acylthioureas and respective primary amines, including five R~1C(O)N=C(NHR~2)_2 with balanced arms(denoted as R~1–R~2–R~2: Ph–Ar'–Ar', L~1(1); Ph–Ar'–Ar', L~2(2); 1-Naph–Ar'–Ar', L~3(3); 1-Naph–Ar'–Ar', L~4(4); 2-Naph–Ar'–Ar', L`5(5); Ar' = 2,6-Me_2C_6H_3, Ar' = 2,6-iPr_2C_6H_3) and three R~1C(O)N=C(NHR~2)NHR~3 with unbalanced arms(denoted as R~1–R~2–R~3: Ph–Ar'–Ph, L~6(6); Ph–Ar' –Ph, L~7(7); Ph–Ar' –Ar', L~8(8)). Treatment of L~(1~5)(1~5) with copper acetate in a molar ratio of 2:1 in dichloromethane led to the formation of homoleptic Cu(Ⅱ) complexes trans-L_2~(n')Cu(9~13), in which the Cu(Ⅱ) center was stabilized by deprotonated ligands Ln'(n = 1~5) in the O,N-bidentate mode. When similar reactions of L~6(Ph–Ar'–Ph)(6) and L~7(Ph–Ar'–Ph)(7) that contain unbalanced arms were investigated, the Cu(Ⅱ) products trans-L_2~(6')Cu(14) and trans-L_2~(7')Cu(15) were formed by deprotonating the bulky amine groups in Ln(-NHAr' for L~6 and-NHAr' for L~7) rather than the-NHPh group. In sharp contrast, trans-L_2~(8')Cu(16) was obtained from two-arm unbalanced L~8(Ph–Ar'–Ar')(8) not by deprotonating the more bulky-NHAr' group but the relatively less bulky-NHAr' group. In a further exploration, the reaction of 1:1 mixed ligands Ln and Lm with copper acetate was found to give only homoleptic Cu(Ⅱ) complex L_2~(n')Cu instead of the heteroleptic one L~(n')CuL~(m'). The in vitro antibacterial activity of L~n was evaluated against S. aureus, E. coli and C. albicans by determining the minimum inhibitory concentrations(MICs) using Kirby-Bauer test.    

3.  A new facile approach to N-alkylpyrroles from direct redox reaction of 4-hydroxy-l-proline with aldehydes  
   ZhiQin Zou  ZeJun Deng  XinHong Yu  ManMan Zhang  SiHan Zhao  Ting Luo  Xin Yin  Hui Xu  Wei Wang《中国科学:化学(英文版)》,2012年第55卷第1期
   An unprecedented acetic acid-catalyzed efficient access to N-alkylpyrroles from reaction of 4-hydroxy-L-proline with a variety of aldehydes has been achieved in good to excellent yields under mild reaction conditions.    

4.  A Short and Stereoselective Synthesis of the (-)-(5R, 6S)-6-Acetoxy-hexadecane-5-olide  
   BinSUN LiZengPENG XueSongCHEN YuLinLI YingLI《中国化学快报》,2004年第15卷第10期
   (-)-(5R, 6S)-6-Acetoxyhexadecan-5-olide 1, a natural mosquito attractant pheromone,was synthesized from readily available aldehyde 2 and cyclopentanone 3 using L-proline-catalyzed asymmetric aldol reaction as the key step.    

5.  Synthesis and Antimicrobial Studies of Novel Billogical Heterocycles  
   PATEL Navin B.  RATHOD Rahul D.《中国化学》,2008年第26卷第12期
   The synthetic route of sildenafil promoted us to synthesize new object molecules. New analogues containing a 4-thiazolidinone ring bonded to the phenyl moiety at the 2-position, 7-(substituted anilino)-6-fluoro-2-(p-meth- oxy-m-{[2-(p-hydroxyphenyl)-4-oxo-1,3-thiazolidin-3-yl]aminocarbonyl}phenylsulfonamido)benzothiazoles (4a—4l) have been synthesized by cyclization with thioglycollic acid of Schiff bases 3a—3l from corresponding 7-(substituted anilino)-6-fluoro-2-(p-methoxy-m-hydrazinocarbonyl phenylsulfonamido)benzothiazoles (2a—2l). Compounds 2a—2l in turn were prepared by dehydroxyhalogenation followed by condensation with hydrazine hydrates of acids 1a—1l. Compounds 1a—1l in turn were prepared by chlorosulfonation of o-methoxy benzoic acid followed by condensation with 6-fluoro-7-(substituted anilino)-2-aminobenzothiazoles. Final compounds have been characterized by their elemental analysis, IR, NMR and mass spectra. All the synthesized compounds have been screened for their antimicrobial activities. Some of them showed good activities.    

6.  Synthesis of substituted 1,2-benzoquinones and substituted 3-hydroxy-4 (1H) -pyridinones: Application of oxidation-Michael addition in organic synthesis  
   李苗盛  马林  张小春  黄志纾  肖韶华  古练权《中国化学》,1999年第4期
   Catechol (1) and 2-ethoxy-2-ethyl-3-hydroxy-4(1H)-pyridinone (4) derivatives can be oxidized to give ortho-quinone of 1,2-benzoquinone (2) and 2-ethoxy-2-ethyl-l,2(2H)-pyridine-3,4-dione (5) that subsequently undergo Michael addition with nucleophiles. This reaction served a convenient route to synthesize 4,5-disubstituted-l,2-benzoquinones (3a-c) and 6-substituted-3-hydroxy-4(1H)-pyridinones (6a-f) .    

7.  Synthesis of homochiral spiro[4.4] nonane-1,6-diols  
   蒋耀忠  鄢明  孙健  胡文浩  李智  宓爱巧  陈新滋《中国化学》,1998年第3期
   Homochiral cis,cis-; cis,trans- and trans,trans-spiro[4.4]nonane-1,6-diols were prepared via diastereoselective reduction of enantiomerically pure spiro[4.4]nonane-1,6-dione (1) with the corresponding reducing agents: lithium n-butyldiisobutylaluminium hydride for cis,cis-diol (2) with 88% yield; BH3·THF for cis, trans-diol (3) with 91% yield; LiAlH4 for trans,trans-diol (4) with 15% yield.    

8.  Novel Method for the Enantioselective Synthesis of β-Lactams  
   YUAN Qing JIAN Shan-zhong WANG Yan-guang《高等学校化学研究》,2008年第24卷第1期
   A novel method for the enantioselective synthesis of β-lactams is described in this study. 2,3-Dihydrobenzooxazin-4-one derived from salicylamide and L-menthone was used as the chiral auxiliary, which reacted with a-bromo-acyl bromides in the presence of pyridine to give carboximides 2. The stereo-controlled Reformatsky-type reactions of carboximides with imines yielded the corresponding trans β-lactams with high enantioselectivities(e.e. 75%-86%) and high chemical yields(63%-85%), meanwhile, the chiral auxiliary dihydrobenzooxazin-4-one was released and recovered.    

9.  Synthesis and Crystal Structure of 2-Fluoro-4-methyl-3-oxo-4-aza-5α-androst-1-ene-17β-carboxylic Acid Methyl Ester  
   JANG  Yin-Zhi XIANG  Zuo LIANG  Da-Wei《结构化学》,2010年第29卷第4期
   Synthesis and Crystal Structure of 2-Fluoro-4-methyl-3-oxo-4-aza-5α-androst-1-ene-17β-carboxylic Acid Methyl EsterJANG Yin-Zhi XIANG Zuo LIANG Da-Wei (Department of Applied Chemistry, Zhejiang Sci-Tech. University, Hangzhou 310018, China)The title compound VII, 2-fluoro-4-methyl-3-oxo-4-aza-5α-androst-1-ene-17β-carboxylic acid methyl ester (C21H30FNO3, Mr = 363.46), was prepared through a seven-step reaction from pregnenolone, and characterized by elemental and single-crystal X-ray diffraction analyses as well as IR, MS and 1H-NMR spectra. It is of monoclinic system, space group P21/c with a = 6.3882(7), b = 9.9033(11), c = 15.4925(17) , β = 91.923(2)°, V = 979.57(19) 3, Z = 2, Dc = 1.232 mg/m3, μ = 0.088 mm-1, F(000)= 392, R = 0.0465, wR = 0.0989 and λ(MoKα) = 0.71073 . The structure indicates that the four cycles (A: C(1)-C(2)-C(3)-N(1)-C(5)-C(10), B: C(5)-C(6)-C(7)- C(8)-C(9)-C(10), C: C(8)-C(14)-C(13)-C(12)-C(11)-C(9), D: C(14)-C(15)-C(16)-C(17)-C(13)) are in chairand trans-configurations. The results of crystal structure determination show that there exist weak intra-molecular hydrogen bonds, resulting in a two-dimensional supramolecular frame-work of the title compound.fluoro-sterol, synthesis, crystal structure, supramolecule    

10.  A CONVENIENT SYNTHESIS OF FLUORINE-CONTAINING QUINOLINES  
   《中国化学快报》,1992年第8期
   2-Fluoroalkyl-4-hydroxy-quinolines were easily obtained from thereactions of 2-(F-alkyl)acetates with aromatic amines in the presence ofEt_3N,followed by cyclization of the intermediates with PPA.    

11.  ENANTIOSELECTIVE TOTAL SYNTHESIS OF 6R-(-)-MASSOIALACTONE  
   《中国化学快报》,1993年第1期
   4'R, Z, 2-(4'-hydroxy-2'-nonenyl)-1,3-dioxane 2 which is an intermediate in the synthesis of chiral δ-lactones, has been syntheslzed from dlepoxide 3. Enantioselective total synthesis of 6R-(-)-massoialactone 1 has been achieved from 2 through 4 steps    

12.  SYNTHESIS OF 3-BUTYLIDENE-5-HYDROXYPHTHALIDE  
   《中国化学快报》,1993年第4期
   3-Butylidene-5-hydroxyphthalide(1)was prepared from 4-hydroxy-benzoic acid(2).    

13.  Synthesis of dimethyl 3-perfluoroalkyl-4-(3-oxo-2-triphenyl-phosphoranylidenbutanylidene)-pent-2-enedioate and its cyclization  
   DING  Wei-Yu CAO  Wei-Guo YAO  Yuan ZHU  Zhong-Mei Department of Chemistry  Shanghai University of Science and Technology  Shanghai 201800  China《中国化学》,1995年第5期
   The title compounds 5a-5c were prepared via the reaction of methyl 2-perfluoroal-kynoates (4) with methyl 5-oxo-4-(triphenylphosphoranylidene)hex-2-enoate (3), which was obtained from the reaction of methyl propynate (2) with acetylmethylenetriphenylphosphorane (1) at -5-0℃. Intramolecular elimination of Ph3PO took place when compound 5 was heated in aqueous methanol at 115-120℃ in sealed tube, yielding dimethyl 2-trifluoromethyl-4-methylisophthalate (6a) from 5a and methyl 5-acetyl-4-hydroxy-2-heptafluoropropanylbenzoate (6b) from 5b, respectively. The structures of compounds 5, 6a and 6b were confirmed by IR, MS, 1H NMR, 19F NMR and 13C NMR spectroscopy and elemental analyses. Rection mechanisms for the formation of compounds 5, 6a and 6b were proposed.    

14.  Synthesis of 1-Benzoyl-3-aryl-4-hydroxy-4-phenylimidazolidin-2-thiones  
   曾润生 邹建平 穆学军 沈琪《中国化学》,2003年第21卷第12期
   l-Benzoyl-3-aryl-4-hydroxy-4-phenylimidazolidin-2-thiones can be synthesized readily from the cyclization of 1-benzoyl-3-arylthioureas with bromine-acetophenone in the presence of excess triethylamiqe.    

15.  Synthesis and Antitumor Activity of Tanshinone Analogues  
   阿吉艾克拜尔·艾萨  吕伟  蔡俊超《中国化学》,2003年第21卷第7期
   8, 8-Dimethyl-5, 6, 7,8-tetrahydrophenanthrene-3, 4-dione (3) and 8, 8-dimethyl-2- ( 1-hydroxy ethyl) -5,6, 7, 8-tetrahydrophenanthrene-3,4-dione (4), two analogues of the antitumor active tanshinone, were synthesized from anisole. The synthesized compounds 3 and 4 were shown to be highly active against leukemia P-388 cell fine as assayed by in vitro MTT method.    

16.  Facile Synthesis of Ureas in lonic Liquid  
   WeiXingQIAN FengYangJU YongMinZHANG WeiLiangBAO《中国化学快报》,2004年第15卷第11期
   The reaction of isocyanates with aliphatic and aromatic amines in the l-n-butyl-3-methylimidazolium tetrafluoroborate (bmimBF4) ionic liquid in good to excellent yields is described.Due to its insolubility, the desired urea solids could be recovered by simple filtration from the ionic liquid after reaction.    

17.  Cochinchin from Dracaena cochinchinensis  
   何兰 王竹红 刘雪辉 方德彩 李华民《中国化学》,2004年第22卷第8期
   A new compound, Cochinchin (1), together with 7,4‘-dihydroxyflavone (2), 7-hydroxy-4‘-methoxyflavane (3),7-hydroxy-3-(4-hydroxybenzyl)chroman (4), 4‘-hydroxy-2,4-dirnethoxydihydrochalcone (5) and 4‘-hydroxy-2,4,6-trimethoxydihydrochalcone (6) was isolated from the resin (trivial name, “dragon‘s blood“) of Dracaena cochinchinensis (Lour.) S. C. Chert. The structure of 1 was elucidated on the basis of spectroscopic data as (2,3-trans)-6-allyl-2-(3,5-dimethoxyphenyl)-3-(4-hydroxyphenyl)-2,3-dihydrobenzo[1,4]dioxin which is a natural product possessing a new framework.    

18.  Synthesis,reactivity and electrochemical properties of substituted cyclopentadienyl cobalt (Ⅲ) complexes  
   侯秀峰  庞震  徐友锋  蔡瑞芳  黄祖恩《中国化学》,2000年第5期
   Cyclopentadienyl cobalt complexes (n5-C5H4R)CoLI2 [L = CO,R=-COOCH2CH=CH2 (3); L=PPh3,R=-COOCH2-CH=CH2 (6); L= P(p-C6H4CH3)3,R=-COOC(CH3) = CH2 (7),-COOCH2C6H5(8),-COOCH2CH = CH2 (9)] were prepared and characterized by elemental analyses,1H NMR,IR and UV-vis spectra.The reaction of complexes (n5-C5H4R)CoLI2[L=CO,R=-COOC(CH3)=CH2 (1) ,-COOCH2C6H5(2):L=PPh3,R =-COOC(CH3)=CH2 (4),-COOCH2C6H5(5)] with Na-Hg resulted in the formation of their corresponding substituted cobaltocene (n5-C5H4R)2Co [R= -COOC(CH3) = CH2 (10),-COOCH2C6H5 (11) ].The electrochemical properties of these complexes 1-11 were studied by cyclic voltammetry.It was found that as the ligand (L) of the cobalt (Ⅲ) complexes changing from CO to PPh3 and P(p-tolyl)3,their oxidation potentials increased gradually.The cyclic voltammetry of α,α'-substituted cobaltocene showed reversible oxidation of one electron pro-    

19.  Chiral Synthesis of 13-Acetyl-12-hydroxy-podocarpane-8,11,13-triene-7-one  
   An Pai LI  Yong Hong GAN  Xiao Shui PENG  Tong Xing WU  Xin Fu PAN* Department of Chemistry  National Laboratory of Applied Organic Chemistry  Lanzhou University  Lanzhou 730000《中国化学快报》,2001年第3期
   Most diterpenoids exhibit significant bioactivities, such as: antibacterial1,2, antider- matophytic2,3, antioxidant4, etc. 13-Acetyl-12-hydroxy-podocarpane-8,11,13-triene-7-one is a diterpene which has been synthesized by Sukumer et al. from the racemic trans isomer 45. Scheme 1Reagents and conditions: i) n-BuLi, n-hexane , r.t., 4 h (70%); ii) 5% Pd/C, ethanol (95%); iii) BF3.Et2O, CH2Cl2, r.t., 12 h (93%); iv) acetyl chloride, anhydrous AlCl3, -5(C, 4 h (90%); v) CrO3/ HOAc/H2O, r.…    

20.  Synthesis and Antibacterial Activity of New Tetracycfic Triazolothiadiazino Fluoroquinolones  
   GuoQiangHU ZhongQuanZHANG WenLongHUANG HuiBinZHANG ShengTangHUANG《中国化学快报》,2004年第15卷第1期
   A series of novel 9-fluoro-10-(4-methylpiperazin-l-yl)-3-substituted-8-oxo-8H-[1,2,4] triazolo[3,4-b]thiadiazino[6,5,4-ij]quinoline-7-carboxylic acids was prepared by a facile synthetic method and the in vitro antibacterial activity against Gram-postive (G^ ) and Gram negative (G^-) bacteria was primarily evaluated.    

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