OPIOID δ RECEPTOR IRREVERSIBLE INHIBITORS 2.SYNTHESIS OF ISOTHIOCYANATE DERIVATIVES OF CARFENTANIL AND 4-METHOXYMETHYLFENTANYL

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OPIOID δ RECEOTIR IRREVERSIBLE INHIBITORS 3.SYNTHESIS OF AMIDE ANALOGHES OF SUPERFIT CARFIT AND METHOFIT

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MOLECULAR STRUCTURE AND ABSOLUTE CONFIGURATION OF SUBEROGORGIN

In the present paper it is reported that the molecular structure and absolute configuration of poisonous suberogorgin are determined by using X-ray diffraction method. The crystal of suberogorgin belongs to orthogonal system with space group D_2~4-P2_12_12_1. The crystallographic parameters are: a=16.135, b=13.189, c=12.901, Z=8. The initial model of the crystal structure was solved by the direct method. The refinement of the strueture parameters was carried out by using the least square method and led to a final R-factor of 0.056. In accordance with the molecular structure of suberogorgin mentioned above, the solvent effect of NMR has been further discussed and the relationship between the molecular structure of suberogorgin and its toxicity has also been preliminarily investigated.     

THE CHOICE OF OPIOID RECEPTOR SUBTYPE IN ISOLATED PREPARATIONS BY OHMEFENTANYL

Ohmefentanyl has significant inhibitory actions on the electrically evoked contractions of guinea pigileum and mouse vas deferens. Their IC_(50) values are 0.15 nM and 0.89 nM, respectively. In the guinea pigileum and the mouse vas deferens, both μ-antagonist naloxone and (μ+κ)-antagonist Mr. 2266 antagonizereadily the agonist action of ohmefentanyl, indicating that ohmefentanyl acts on μ-receptors in the guineapig ileum and the mouse vas deferens. Like other μ-agonists, ohmefentanyl has agonist activity but noantagonist action in the rat vas deferens. In the rabbit vas deferens, the activity of ohmefentanyl is veryweak. The IC_(50) value is 149 nM. These results further indicate that ohmefentanyl is a potent and selectiveμ-agonist.     

MOLECULAR STRUCTURE AND ABSOLUTE CONFIGURATION OF THE DITERPENE LACTONE, PRAELOLIDE

Praelolide is a new compound which was isolated out from the gorgonian, Menella praelonga (Ridley), collected from the South Sea of China at Zhanjiang, Guangdong. The molecular formula is C_(28) H_(35) O_(12)C1. The research result by X-ray diffraction method on the crystal structure is presented. The compound is orthorhombic with space group P2_12_12, cell dimensions α=16.936, b=16.709, c=10.333, and Z=4. The structure has been solved by direct method and refined to R=0.055 for 2257 unique observable reflexions by least-squares. The molecule is composed of the major conformational isomer in which the three main rings(a six-membered ring, an eight-membered ring, a six-membered ring) take separately the form of chair-chairboat-chair, a five-membered actone ring, a C1 substitution, 4 acetate groups, and a three-membered epoxide ring. The absolute configuration of the molecule has also been determined by statistics (R factor ratio =1.012) and Bijvoet pairs observation. For 30 pairs of the greatest anomalo     

SYNTHESIS AND CONFIGURATION OF THE DEGRADATION PRODUCT OF YINGZHAOSU B

Synthesis of the degradation product 2 of Yingzhaosu B wasaccomplished and the configuration was determined.     

SYNTHESIS AND CHARACTERISTICS OF HOMOBINUCLEAR MACROCYCLIC COMPLEXES OF RARE EARTH METAL ISOTHIOCYANATE AND PHENOLIC SCHIFF BASES

Eleven homobinuclear macrocyclic rare earth metal ions complexes are obtained as com-pounds of 2:2 Schiff base formed by condensing 2,6-diformyl-4-tert-Butylphenol and triethy-lenetetramine by a template procedure using rare earth metal isothiocyanates. These complexesare characterized by elemental analyses, FABMS, IR, conductivity and magnetic susceptibility.The variable-temperature magnetic susceptibility (4--300K) of complexes of Gd(Ⅲ) and Tb(Ⅲ) has been determined. A satisfactory fit to theoretical curve derived from spin Hamil-tonian operator was obtained by least squares method. The exchange interaction parameters areJ =-0.220 cm~(-1) for Gd, ,ZJ~?=-0.052 cm~(-1) for Tb. The results indicate a very weak anti-ferromagnetic interaction between Gd~(3+)-Gd~(3+), Tb~(3+)-Tb~(3+) ions.     

SYNTHESIS AND CHARACTERIZATION OF NOVEL MICROPOROUS ALUMINOPHOSPHATES.

A series of novel aluminophosphates,named AlPO_4-CJ_n(n=2-5),has beensynthesized hydrothermally from R-Al_2O_3-P_2O_5-H_2O systems(R=organic amine molecules),and characterized by means of X-ray powderdiffraction,infrared,SEM,XPS,composition and thermal analyses.     

SYNTHESIS AND CHARACTERIZATION OF POLYBENZOTHIAZOLAMIDES

Aromatic polybenzothiazolamides were prepared by low temperature solution method by condensing the 2, 2'-diarnino-6, 6'-bibenzothiazole with four different acid chlorides in quantitative yield. These polymers were characterized by IR and NMR. Viscosities of these polyamides range from 0.42 to 1 dl/gm. All these polymers were stable upto 300℃in air.     

1-SUBSTITUTED PHENYL-β-CARBOLINES:SYNTHESIS AND SPECIFIC BINDING WITH BENZODIAZEPINE RECEPTOR

By the condensation of tryptamine with appropriate substituted benzalde-hyde followed by Pictet-Spengler reaction,a series of 1-aryl-tetrahydro-β-carbo-lines(THβCs)were obtained.After dehydrogenation using sulfur,Pd-C or lead te-traacetate(LTA),these THβCs can give the corresponding β-carbolines(βCs)whichexhibit specific binding with rat brain benzodiazepine receptor in vitro.     

SYNTHESIS AND CHARACTERIZATION OF COMB-SHAPED POLYBUTADIENES

Polybutadiene (PB) was chlorinated with t-BuOCl without chain crosslinking and degradation togive chlorinated polybutadiene (Cl--PB) with active allylic chlorine atoms on the backbone. Comb-shaped PB was prepared by coupling of Cl--PB with "living" PB anions in a mixed solvent of cyc-lohexane and tetrahydrofuran. Characterization by GPC and osmometry showed that purifiedproducts were welldefined comb-shaped PB composed of low polydispersity backbone chain andrandomly distributed grafts of uniform length. The averagr number of branches could be variedin a wide range to meet the needs of structure-properties relationship studies.     

SYNTHESIS AND CHARACTERIZATION OF POLYURETHANE LATEX

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SYNTHESIS AND CHARACTERIZATION OF 1-NAPHTHYLMETHYL METHACRYLATE-METHYL METHACRYLATE COPOLYMERS

A series of 1-naphthylmethyl methacrylate (NMMA)-methyl methacrylate (MMA) copolymerswere synthesized on free radical mechanism. The reactivity ratios of NMMA (r_1) and MMA (r_2) werereported to be 0.83 and 0.89, respectively. The characterization of the copolymers by using IR, NMR,GPC, UV and fiuorescence spectrometry was described in this paper.     

ASYMMETRIC SYNTHESIS OF STEROID CD-RING SYNTHON AND APPLICATION TO SYNTHESIS OF STEROIDS

D-norgestrel 1 has been synthesizedfrom an optically active synthon 3 whichwas prepared from 13-ethyl-8, 14-seco ster-oid 2 by microbial asymmetric reductiond,Optically active synthon 4 obtained fromthe cyclization of the symmetric triketone     

AN AB INITIO STU DY ON THE CORELATION BETWEEN THE ABSOLUTE CONFIGURATION AND THE CD SPECTRA OF ORGANIC PEROXIDES

Correlation between the absolute configuration and the CDspectra of organic peroxides was studied by ab initio method with a mo-d el moleeule CH_3-O-O-CH_3.For P form when 0°≤θ(twist angle of C-O-O-C)<90°, there is positive Cotton effect;when 90°<θ≤180°, there is nega-tive Cotton effect;the curve is bisignate at θ=90°.     

SYNTHESIS AND CRYSTAL STRUCTURE OF NEODYMIUM COMPLEX OF 1-METHYL-1,4,7,10-TETRAAZACYCLODODECANE

The complex [Nd(L)(CH_3CN)(CF_3SO_3)_3] has been synthesized, where L=1-methyl-1,4,7,10-tetraazacyclododecane. The crystal structure of the complex has been determined by a fourcircle X-ray diffractometer to a final R value of 0.0370 and Rw value of 0.0385 respectively. The crystal is triclinic system, space group P1 with a=8.738(2), b=12.870(3), c=12.900(3), α=85.63(2), β=87.25(2), γ=78.30(2)°, V=1415.71(60)~3, Z=2, Dc=1.92g/cm~3. The neodymiumion is eight-coordinated, forming a distorted square antiprism.     

SYNTHESIS AND CHARACTERIZATION OF N-（1-NAPHTHYL） SUCCINIMIDE

In this paper a modified two-step procedure for synthesis of N-（1-naphthyl） suecinimide （NaS） was developed, and the molecular structure of NaS was properly characterized by XRD, FT-IR, 1H NMR, DSC, etc. The results show that the melting point of our product is 159 ℃-160.5 ℃, and the characteristic infrared absorption band of carbonyl group splits into two peaks （1705cm^-3/1779cm^-3）, which are found to be quite different from the documented data （rap 147℃ -149℃; IR C=0-1700cm^-3）. Besides, photophysical spectroscopy was found to be powerful to study the molecular structure and crystal morphology of NaS compound.     

SYNTHESIS AND SEMIEMPIRICAL CALCULATIONS OF THIAZOLIDINONE AND IMIDAZOLIDINONE DERIVATIVES OF α-DIONES

The condensation reactions of α-diones with rhodanine and creatinine to give acenaphthylidene, isatylidene and thioisatylidene derivatives, which may act as potential bioactive compounds, are described. The synthesized compounds have been characterized by elemental analysis and spectral studies, as well as by molecular modelling using PCWIN model.     

ABSOLUTE CONFIGURATION OF (-)ANISODINE (A NEW GANGLIO BLOCKING AGENT) AND (-)ANISODINIC ACID

A new tropane alkaloid, (-)anisodlne (Ⅰ), was isolated from the plant of Anisodus tanguticus. It is a novel ganglio blocking agent. The absolute configuration of (-)anisodinic acid (Ⅶ), which-is the side chain of (-)anisodine, was determined by chemical correlation with (R) (-)-2-phenyl-1, 2-propanediol (Ⅳ) and (R) (-)-2-hydroxy-2-phenylpropionic acid (Ⅵ). Thereby (-)anisodine with the absolute configuration shown as (Ⅰ) is 6β, 7β-epoxy-1αH, 5αH-tropan-3α-ol (S) 2'-phenyl-2', 3'-dihydroxypropionate. Two new tropane alkaloids: 6β, 7β-epoxy-1αH, 5αH-tropan-3α-ol 2',3'-epox-ypropionate (Ⅲ) and 2'-phenyl-2'-hydroxypropionate (Ⅴ) were prepared and its physical constant is reported in this paper.     

SYNTHESIS AND PROPERTIES OF NEW INTERPOLYMERIC COMPLEXES

β-(2-imidazolinyl)-ethyl methyl diethoxy silane quarternary halides and its condensed polymers with bisphenol A were synthesized and characterized. The polycation-polyanion complexes were prepared by the condensed polymers and poly (styrene sulfonate). The solubility and thermal stability of interpolymeric complexes were investigated.