The synthesis of anthracyclinones-ii : The synthesis of 7,9-bisdeoxycarminomycinone and -daunomycinone

7,9-Bisdeoxycarminomycinone has been synthesised from 5-hydroxyquinizarin by two annelation routes involving nitronate addition to C-2 and aldol condensation at C-3. 4-Demethoxy-7,9-bisdeoxydaunomycinone has been synthesised efficiently by similar methods.     

The synthesis of dl-coriolin

The synthesis of dienone $\text{2}$, which has previously been converted into the title compound in one step, is described. The methanoindene $\text{7}$ is transformed into dienone-alcohol $\text{58}$ in eighteen steps (12% overall yield). This was then hyaroxylated at C-8, using the known method, to afford key dienone $\text{2}$.     

艾托拉嗪的合成

自从色洛托宁(Serotonin)在1948年作为神经传导素被发现以后,它就与中枢神经系统(CNS)的活动联系在一起.经过科学家们的多年努力,芳基哌嗪作为种类繁多的5-HT1A受体中的一类得到了迅速发展,像布斯哌隆(Buspirone)和伊沙匹隆((Ipsapirone)很早就作为有效的抗焦虑和抗抑郁症药物得到广泛的应用.     

The synthesis of fexofenadine

This work proposes a new simple route for fexofenadine synthesis with low cost and easily obtainable raw materials. We use benzene and methallyl as starting reactants, applying steps of Friedel–Crafts alkylation reaction, hydrolysis, oxidation, esterification reaction, and reduction reaction to obtain the intermediate product, followed by N-alkylation reaction to obtain 4-{1-hydroxy-4-[4-(hydroxydiphenyl)-piperidine]butyl}-α,α-dimethylbenzene acetate. Then, the final product fexofenadine is obtained upon hydrolysis. In the synthesis process, we constantly optimize the reaction conditions such as reaction time, reaction temperature, solvent selection, and other factors, thus improving the final yield of the target product fexofenadine to 33.51 %.     

The synthesis of pyrimidoaporphines

The reaction of 1-benzyl-3,4-dihydroisoquinolines with ethoxycarbonyl isocyanate yields exclusively the N-acylated product 2. Thermal rearrangement of these enamides at 108° C. yields the pyrimidoisoquinolines 3 which may be alkylated or ethoxycarbonylated exclusively on the pyrimidone nitrogen. The pyrimidoisoquinolines possess a stilbene chromophore and are capable of undergoing the stilbene-phenanthrene conversion. Thus irradiation of 3 in the presence of iodine as a dehydrogenating agent yields the novel pyrimidoaporphine nucleus (7-9) in good yield.     

The synthesis of d-C-mannopyranosides

This article reviews the different methods and highlights the general trends that have been developed to selectively obtain α- or β-d-C-mannopyranosides.     

The synthesis of polyfluoroalkoxylbenzaldehydes

Several polyfluoroalkoxyl benzaldehydes were synthesized from the nucleophilic reaction between polyfluoroalkanesulfonate and various sodium phenolates with cetyltrimethylammonium bromide or tetrabutylammonium bromide as PTC. The yields were in the range of 55%–70%. Using a modified procedure Cl(CF₂)₂SO₂Cl was prepared from ClCF₂CF₂I with an improved yield of 91% and was used to synthesize the polyfluoroalkanesulfonate 2'.     

The synthesis of hydroxyphenylthiophenes

The synthesis of the five isomeric methoxyphenylthiophenes is described. The methoxy compounds were hydrolyzed to yield the hydroxyphenylthiophenes.     

The synthesis of dinaphthothiophenes

The synthesis of dinaphtho[1,2-b:2′,3′-d]thiophene ( 6 ), dinaphtho[2,1-b:2′,3′-d]thiophene ( 15 ), dinaphtho-[1,2-b:1′,2′-d]thiophene ( 20 ), dinaphtho[2,1-b:1′,2′-d]thiophene ( 26 ), dinaphtho[2,3-b:2′,3′-d]thiophene ( 37 ) and dinaphtho[1,2-b:2′,1′-d]thiophene ( 45 ) has been accomplished.     

The synthesis of metacycloprodigionsin

Metacycloprodigiosin 1, a tripyrrole pigment isolated from Streptomyces longisporus ruber, has been synthesized by condensation of the meta-fused pyrrole 2, prepared from cyclododecanone, with the known methoxybipyrrole aldehyde precursor 3.     

The synthesis of vinylpyrrolidone

Summary The synthesis of vinylpyrrolidone from succinic acid was accomplished without the use of acetylene or increased pressure.     

The synthesis of zinniol

Zinniol 10, 3 - methoxy - 4 -methyl - 5 (3 - methyl - 2 - butenyloxy) - 1,2 - benzenedimethanol, a metabolite isolated from the pathogenic fungus Alternaria zinniae, has been synthesised.