2-甲基-6-对甲苯基-1,6-庚二烯的合成

以对甲苯乙酮(1)为原料,经烯醇硅醚化,Lewis酸催化Michael加成反应和Wittig反应,合成了新倍半萜烯化合物2-甲基-6-对甲苯基-1,6-庚二烯。     

Recent developments in the chemistry of perhydroindoles and perhydrocinnolines

Recent synthetic routes to the tetrahydro, hexahydro and octahydro derivatives of indoles are reviewed. An interesting one is the formation of 3-amino-4-oxo-4,5,6,7-tetrahydroindoles in the reaction of 2-phenacyl cyclohexane-l,3-diones with 1,1-disubstituted hydrazines. Antifertility, cns depressant and antiinflammatory activities have been encountered for perhydroindoles besides other biological activities. Hexahydrocinnolines are obtained from the reaction of 2-phenacyl (acetonyl) cyclohexanones and cyclohexane-1,3-diones with hydrazines, while octahydrocinnolines are formed from cyclohexanone-2-acetic acids and hydrazines in two steps. 5-oxo-5,6,7,8-hexahydrocinnolines and their oximes undergo anomalous and interesting aromatisation reactions. Some hexahydrocinnolines are cns depressants while octahydrocinnolines are analgesics. More importantly, they are precursors for interesting azamorphinans. Contribution No. 736 from Research centre     

Fungicidal,bactericidal and antifertility activities of diorganosilicon(IV) complexes derived from benzothiazolines

Synthetic, structural and biological aspects of trigonal-bipyramidal, Me₂S(N—S)CI and octahedral, Me₂Si(N—S)₂ types of diorganosilicon(IV) complexes of heterocyclic benzothiazolines (N—SH) are described. The complexes were characterized by elemental analysis, molecular weight determination, conductance measurements and electronic, infrared, ¹H and ¹³C NMR spectroscopic studies. Some ligands and their corresponding dimethylsilicon(IV) complexes have been tested for their effects on several pathogenic fungi and bacteria and found to be quite active in this respect. Antifertility activity in male mice of some representative ligands and their silicon complexes was also evaluated and discussed.     

Antifungicidal,antibacterial and antifertility activities of biologically active heterocyclic thiosemicarbazones and their coordination complexes with the dimethylsilicon moiety

Synthetic, structural and biological aspects of trigonal-bipyramidal, Me₂Si(NS)Cl and octahedral, Me₂Si(NS)₂ types of organosilicon (IV) complexes of heterocyclic thiosemicarbazones (N? SH) have been described. The complexes were characterized by elemental analysis, molecular weight determination, conductance measurements and electronic, infrared, ¹H and ¹³C NMR spectral studies. Some ligands and their corresponding dimethylsilicon (IV) complexes have been tested for their effects on several pathogenic fungi and bacteria. Two representative complexes have also been found to act as sterilizing agents by reducing the production of sperm in male mice.     

Toxicological effects,biological aspects and spectral characterization of organoboron(III) complexes of sulfonamide‐imines

The toxicological effects, biological aspects and spectral characterization of organoboron(III) complexes of sulfonamide‐imines derived by the condensation of salicylaldehyde with different sulfa‐drugs are described. The benzene‐soluble, high‐molecular‐weight complexes have been characterized using a wide range of analytical and spectroscopic techniques, viz. UV, IR, ¹H and ¹¹B NMR. On the basis of these studies, it is inferred that the imines derived from sulfa drugs and salicylaldehyde behave as dibasic tridentate ligands and thus provide a tetrahedral environment around the boron atom. Finally, all these complexes have been screened for their antimicrobial activity against a variety of fungal and bacterial strains and their toxicological effects on male albino rats examined at the dosages employed. Copyright © 2004 John Wiley & Sons, Ltd.     

Intramolecular phenylborane complexes with monobasic bidentate Schiff bases

A series of intramolecular complexes with Schiff base ligands having N∩S and N∩O donor systems were synthesized in an open vessel under microwave irradiation (MWI) using a domestic microwave oven. The reaction time has been brought down from hours to seconds with improved yield as compared with the conventional heating. The complexes have been characterized on the basis of elemental analysis, conductance measurements and spectroscopic analysis. Based on the IR, ¹H NMR, ¹¹B NMR and ¹³C NMR spectroscopic studies, a tetrahedral geometry has been proposed for the resulting complexes. The compounds have been screened in vitro against bacteria and fungi to test their antimicrobial property and in vivo in male albino rats to test their antifertility property. The testicular sperm density, motility and density of cauda epididymal spermatozoa along with biochemical parameters of reproductive organs have been examined and discussed. Copyright © 2007 John Wiley & Sons, Ltd.     

Crystal structure of 17-oxo-5α-androstano [3,4-C] 1′2′5′-oxadiazole (HS1000)

The title compound (C₁₉H₂₆N₂O₂) is one of a series of novel heteroatom steroidal derivatives recently prepared for testing their antifertility profiles and progesterone binding affinity. It is one of a pair of epimers differing in configuration at position 5. The X-ray analysis has uniquivocally resolved this ambiguity. The compound crystallizes in space group P2₁2₁2₁, a = 9.257(3), b = 9.419(3), c = 19.089(5)Å, and Z = 4 and the structure was solved by direct methods. In the steroid skeleton Ring A does not exhibit the chair conformation commonly found in the steroid nucleus, being considerably strained, presumably as a consequence of the fused planar oxadiazole ring E. Rings B and C, however, are chairs and ring D is in an intermediate envelope/half-chair conformation. All rings of the steroid skeleton are trans connected.     

Syntheses,silylation, characterization,and antimicrobial and antifertility activities of organoboron derivatives of some bioactive monofunctional bidentate semicarbazones

Some new mononuclear organoboron derivatives of the type PhBL^1–5(OH) ( 1a – 1e ) were synthesized by the reaction of PhB(OH)₂ and LH (LH = OC(NH₂)NH:NC(CH₃)₄C₆H₄R, where R = H (L¹H); CH₃(L²H); OCH₃(L³H); Cl (L⁴H); Br (L⁵H)) in 1:1 molar ratio in refluxing tetrahydrofuran (THF). This was followed by the reactions of PhBL^1–5(OH) with NH(SiMe₃)₂ in 2:1 molar ratio in THF to yield new heterodinuclear derivatives of the type PhBL^1–5(OSiMe₃) ( 2a – 2e ). All these newly synthesized complexes were characterized using elemental analyses and their probable structure was proposed on the basis of infrared, ¹H NMR, ¹³C NMR, ¹¹B NMR and ²⁹Si NMR spectral data and mass spectrometry. Semicarbazone ligands and their corresponding mono‐ and heterodinuclear boron derivatives were screened against pathogenic bacteria (E. coli and P. aeruginosa) and fungi (A. niger and P. peniculosum) to examine their antimicrobial activities. Representative compounds of each series of mono‐ and heterodinuclear boron derivatives and a ligand were screened for their antifertility activity on male adult Wistar rats.