Isolation and Crystal Structure of 1′,4′-Trans-diol of Abscisic Acid

1 ′,4′-Trans-diol of abscisic acid was isolated from botrytis cinerea as a colorless crystal. The molecular and crystal structures have been determined by X-ray diffraction analysis. It crystallizes in orthorhombic system, space group P212121 with a = 6.724(3), b = 17.559(6), c =12.265(2) (A), a = β = y = 90°, V = 1448.1(8) (A)3, Z = 4, Dx = 1.222 g/cm3, F(000) = 576 and μ(MoKa) = 0.087 mm-1. The final R = 0.0628 and wR = 0.1604 for 2501 independent reflections with Rint = 0.0160 and 1679 observed reflections with I ＞2σ(Ⅰ). There are three intermolecular hydrogen bonds in a unit cell.     

The Peculiar Existence of Protein-Bound Unconjugated Bile Acid in the Cytoplasmic Fraction of Rat Brain

Bile acids are synthesized in the liver from cholesterol by the action of hepatic enzymes and excreted into the small intestine via the bile duct. In the intestinal lumen, they assist lipolysis and the absorption of fats by forming mixed micelles, and then return to the liver upon absorption in the     

Crystal Structure of Sar1[H79G]-GDP Which Provides Insight into the Coat-controlled GTP Hydrolysis in the Disassembly of COP Ⅱ

1 INTRODUCTION The selective export of cargoes from the endore- ticulum is an evolutionarily conserved function cen- tral to cell development and proliferation. This ex- port is regulated by the Sar1 GTPase, a member of the Ras superfamily of small GTPases[1~4]. Like other Ras proteins, Sar1 functions as binary switches by cycling between inactive GDP- and active GTP- bound states[5]. The conversion of Sar1-GDP to Sar1- GTP following receptor activation is catalyzed by guanine nu…     

Preparation and antibacterial activity of aromatic derivatives of β-aminopropionic and γ-aminobutyric acid

Ten aromatic derivatives of β-aminopropionic acid and γ-aminobutyric acid were prepared.Their compositions and structures were identified by elemental analysis,IR,and 1H NMR.They have been examined for their antibacterial action against Staphylococcua aurens and Escherichia coli.These compounds showed higher activity than the aromatic derivatives of ct-amino acid which were reported previously.The general conclusion to be drawn is that the distance between amino and carboxylic group in these molecules could affect their antibacterial activity.Furthermore,those compounds with p-methyl substituent in phenyl ring exhibit higher activity than the others,and all the compounds exhibit higher activity against Escherichia coli and against Staphylococcua aureus.     

A Facile Synthesis of N-Substituted Spirocyclic Diester of α-Aminophosphonic Acid

Inl965,RudietaL1rePortedthataspirocycliccompound(3,9-2H-2,4,8,lO-tetraoxa-3,9-diphosPhasPirol5,5lundecane-3,9-disulfide)possessesverygoodherbicidalactivity.Ourrecentresearchzshowedthatsomeix-andnophosphonicacidderivativesalsoexhibitgoodherbicidalachvity.Inaddition,ChrisMeierrecentlyreportedtiutafterfor-mationoftheprodrugwithacyclicphosphorylgroup,thebiologicallyactivenucleosideanalogUewouldovercomethedifficultyoftheintr8cellulardeliverybecauseitiseasierfortheprodrugtopassthrougl1amembranet…     

A convenient synthesis of 2β,3α-dihydroxyurs-12-en-28-oic acid as a natural diastereoisomer of corosolic acid

2β,3α-Dihydroxyurs-12-en-28-oic acid（6） is a naturally occurring diastereoisomer of corosolic acid with glycogen phosphorylase inhibitory activity.A new strategy for the semi-synthesis of 6 was developed.Using the commercially available ursolic acid（1） as the starting materials,6 was synthesized through five facile reactions with a high stereoselectivity and an overall yield of 47.3%.The structure of 6 was confirmed by optical rotation.ESI-MS,¹H NMR and ¹³C NMR data.     

Hydroxylation of nigranoic acid to 6β-hydroxynigranoic acid by Caryospora carllicarpa YMF1.01026

Microbial transformation of nigranoic acid by Caryospora carllicarpa YMF1.01026 afforded the new derivative 6β-hydro-xynigranoic acid. Its structure was elucidated by spectroscopic methods.     

An Efficient Synthesis of Heterocyclic Substituted Ureidoalkylphosphonates

Inarecentreport',a-aminoalkylphosphonateswithpyrazoIemoietyshowedverygoodinhibitoryeffectsagainstplantvirus.Inaddition,a-aminoalkylphosphonicacidsserveforinhibitingenZymeactivity,bacterialgrowthandinagrochemistryasantifungalagents,herbicidesandplantregulators'.Thereforeconsideringthewideapplicationsofsuchcompoundsandthebioactivitiesofheterocycliccompoundsandureaderivatives,wedesignedtosynthesizealargevarietyofheterocyclicsubstitutedureidoalkylphosphonates3.Thereportedmethodforsynthesisofsubst…     

Design and synthesis of chiral single-armed molecular tweezers derived fromα-hyodeoxycholic acid

A novel type of molecular tweezers with different chiral center and cleft has been designed and prepared by usingα-hyodeoxycholic acid as spacer and D/L-amino acid methyl ester as chiral arm attached at 3-position.Their structures were elucidated by ~1H NMR,FTIR and elemental analysis.Their recognition properties for various D/L-amino acid methyl esters were also investigated.The preliminary results indicated that these chiral single-armed molecular tweezers exhibited good recognition ability for D/L-ami...     

Crystal Structure of Nicotinic Acid·3,5-dinitrobenzoic Acid Organic Adduct

1INTRODUCTIONThedevelopmentofhighlyefficientnonlinearoptical(NLO)crystalsforvisibleandultraviolet(UV)regionsisextremelyimportantforbothlaserspectroscopyandlaserprocessing.Themainmeritsoforganicmaterialscomparedwithinorganiconesforsuchsecond-harmonicgenera…     

Synthesis of palladium-rhodium bimetallic nanoparticles for formic acid dehydrogenation

Herein,we report for the first time the synthesis of preformed bimetallic Pd-Rh nanoparticles with different Pd:Rh ratios(nominal molar ratio:80-20,60-40,40-60,20-80) and the corresponding Pd and Rh monometallic ones by sol immobilization using polyvinyl alcohol(PVA) as protecting agent and NaBH4 as reducing agent,using carbon nanofibers with high graphitization degree(HHT) as the desired support.The synthesized catalysts were characterized by means of Transmission Electron Microscopy(TEM) and inductively coupled plasma optical emission spectroscopy(ICP-OES).TEM shows that the average particle size of the Pd-Rh nanoparticles is the range of 3-4 nm,with the presence of few large agglomerated nanoparticles.For bimetallic catalysts,EDX-STEM analysis of individual nanoparticles demonstrated the presence of random-alloyed nanoparticles even in all cases Rh content is lower than the nominal one(calculated Pd:Rh molar ratio:90-10,69-31,49-51,40-60).The catalytic performance of the Pd-Rh catalysts was evaluated in the liquid phase dehydrogenation of formic acid to H2.It was found that Pd-Rh molar ratio strongly influences the catalytic performance.Pd-rich catalysts were more active than Rh-rich ones,with the highest activity observed for Pd90:Rh10(1792 h^-1),whereas Pd69:Rh31(921 h^-1) resulted the most stable during recycling tests.Finally,Pd90:Rh10 was chosen as a representative sample for the liquid-phase hydrogenation of muconic acid using formic acid as hydrogen donor,showing good yield to adipic acid.     

Synthesis of unnatural N-glycosyl α-amino acids via Petasis reaction

A convenient and efficient protocol for the synthesis of unnatural N-glycosyl a-amino acids was developed.Condensation of 1,3,4,6-tetra-O-actyl-β-D-glucosamine hydrochloride,alkenyl boronic acid,and glyoxylic acid was achieved in CH_2C1_2 to give the derivatives of 2-(N-glycosyl)aminobut-3-enoic acid which may find applications in glycobiology research and medicinal chemistry.     

The design and synthesis of a novel organophosphorus compound containing the structure of both β-amino acid and β-aminophosphonate

<正>A novel organophosphorus compound containing the structure of bothβ-amino acid andβ-aminophosphonate is designed and synthesized.Arbuzov reaction with P(OEt)_3,the N-Boc protected iodide 3 cannot provide the desired product but 2-oxazolidinone 4 because of the neighboring-group participation of the Boc moiety.To avoid the intramolecular participation of the carbamates,the Ts protecting group is employed and the Ts-protected iodide 5 affords the target product successfully.     

Syntheses of α-Hydroxyarylacetic Acidsin the Presence of DifferentPhase Transfer Catalysts Under Sonication

IntroductionA one-step preparation of a--hydroxyarylacetic acids from arylaldehydes, bromoform andpotassium hydroxide in the presence of catalyst lithium chloride in a mixed solvent of waterand 1,4-dioxane has been de.cribed[1]. There are a number of articles wherein authors havereported the preparation of a-aminoarylacetic acidsL2.3J and a-hydroxyl c ycloh exaneca r box yl icacid with a similar procedure[']. On the other hand, it was reported that some reactions underultrasonic wave often ta…     

Synthesis of α-Aminoarylacetic Acids in the Presence of Phase Transfer Catalysts

Inearlierpublications""aone-stepphasetransfercatalyzedreactionforpreparingaaminoarylaceticacidsfromarylaldehydesandchloroform,usingquaternarysaltsorf3CDasphasetransfercatalyst,wasdescribed;Itwasalsoreportedthatsomereactionsundersonicationconditionoftenoccurmorerapidlyandeasily'.Wenowfindthatthisreactioncanbeadvantageouslyrealizedbyphasetransfercatalysisundersonication.Optimumreactionconditionsweredeterminedwithbenzaldehyde.Inthepresenceoflithiumchloride,theyieldnoticeablydecreases(seeTablel)…     

Oxalic acid as a simple and efficient organocatalyst for three-component synthesis ofα-amino nitriles

A simple,efficient,and general method has been developed for the synthesis ofα-amino nitriles.Oxalic acid as a BrФnsted acid promotes the addition of TMSCN to various imines(generated in situ).     

Synthesis of Optically Active trans-2-Aminocyclopropanecarboxylic Esters

The research on optical alicyclic β-amino acids has recently attracted increasingly attention due to their significant pharmacological properties endowed by rigid frameworks, stable conformation1. Numerous biologically active peptides, β-lactams and some other natural products2 contain optical alicyclic β-amino acids. Cyclopropyl-modified alanines have been proved to be useful intermediates in medicine synthesis because of their rigid framework and reactive functional groups (amino and carb…     

Study on the Structure of Supramolecular Inclusion Complex of β-Cyclodextrin with Retinoic Acid

The importance of Vitamin A for human health has been stressed in resent studies1, meanwhile its derivative so-called retinoic acid (RA) has been widely used as pharmaceutical to treat several types of skin disease and cancer2,3. However the application of retinoic acid is restrained for its poor water solubility, unstability and side effect on the human body.Cyclodextrins (CDs) are macrocyclic oligosaccharides built up from 6, 7, or 8 glucopyranose units called (, (, and (-CD, respectively…     

Synthesis and Anticonvulsant Activity of γ-Aminobutyric Acid Derivatives

y-Aminobutyricacidisregardedasoneofthemaj0rinhibit0ryneur0transmittersinthemammaliancentralnervoussystem."'UnderPhysiologicalconditi0ns,y-aminobutyricacidpo0riycrossestheb1ood-brainbarrier.SoitisnoteffectivebyoraladministTation.3'4ItisIikelythatan0n-toxicderivativeofy-arninobutyricacidwhichentersthebraineasilywi1lhaveusefultheraPeuticproperties.Withthisinmind,wehavedesignedandsynthesizedl6derivativesofy-aminobubocacidwithaniminelinktoa1ip0philiccarrierinordert0facilitatethepassage0fy-aminobu…     

The structural analysis of the inclusion complex of β-cyclodextrin with m-nitrophenoxyacetic acid

The inclusion complex of β-cyclodextrin with m-nitrophenoxyacetic acid was studied by single crystal X-ray diffraction,2D NMR spectroscopy and semi-empirical methods AMI.The crystallographic study shows that two β-cyclodextrins are held together by hydrogen bonds to form head-to-head dimers.The disordered guest molecule adjusts itself to attain the most stable accommodation into the cavity in which the nitro group is located at the dimer interface while the carboxyl group is buried in the primary hydroxyl groups of β-cyclodextrin.The guest inside the cavity is disordered over two sites and exhibits mobility.Moreover,2D NMR spectroscopy and theoretical study show the same inclusion behavior.In comparison to the inclusion complex of β-cyclodextrin with p-nitrophenoxyacetic acid,the host-guest stoichiometries are different,i.e.,2:1 for m-nitrophenoxyacetic acid and 1:1 for p-nitrophenoxyacetic acid,while the inclusion orientation and the packing pattern of the host are similar in both complexes.