40231-01-4

A series of acetylenic furan derivatives have been synthesized via Pd-catalyzed coupling reactions of 2-(alkyltelluro)furan with several terminal alkynes. These compounds showed good anti-inflammatory activity in the carrageenin-induced rat paw edema assay. This represents a new and efficient method for the synthesis of pharmacologically active compounds.

The invention discloses a kind of type I of the pyrimidine or pyridine pyridine ketone compound and its preparation and application, which belongs to the technical field of pharmaceutical preparation. The compounds have high-efficient and selectively inhibit the cell cycle dependent kinases (Cdks) CDK4 and CDK6 active, and then by inhibiting CDK4/CDK6 prevent tumor cell division. Therefore, the compounds of this invention can be used for CDK4 and CDK6 the involved in cell cycle control disorders result in various diseases, especially suitable for the treatment of malignant tumors. (by machine translation)

Provided herein are new N-,C-disubstituted azoles and derivatives thereof that exhibit nematicidal activity and are useful, for example, in methods for the control of unwanted nematodes.

A novel class of diyne compounds and diyne salts provided herein are effective and potent Olel protein inhibitors, useful for treating fungal pathogens. Compounds, fungicides and methods are provided as novel, potent and broad spectrum antifungal agents for treatment against a wide variety of fungal pathogens in humans and animals, and in the agricultural setting.

Copper-catalyzed cross- and carbonylative coupling reactions have been achieved in the reaction of a variety of alkynyliodonium salts with arylboronic acids and organostannanes under the mild reaction conditions in high yield. Our investigation shows that the alkynylidonium tetrafluoroborates are more efficient than those of triflates and tosylates. Georg Thieme Verlag Stuttgart.

Compounds of the type AZCF=CCl2, prepared from AZA (thiophene, furan, and p-dibromobenzene; Z = 2,5-thiophenediyl, 2,5-furandiyl, and p-phenylene; A = H or Br), were converted into CCl2=CFZCCH, CCl2=CFZCCCF=CCl2, and CCl2=CFZCCSi(CH3)3 in a one-flask procedure via LiZCCLi.The products were further converted into acetylenic compounds such as (CH3)3SiCCZCCSi(CH3)3 and (CH3)3SiCCZCC-CCSi(CH3)3. 1-Ethynyl-4-(1,3-butadiynyl)benzene was izolated. 2,5-Diethynylthiophene and -furan were prepared in two steps from thiophene and furan, respectively, via CCl2=CFZCF=CCl2.By treatment with copper (II) acetate hydrate in pyridine, (CCl2=CFZCC-)2 were obtained not only from CCl2=CFZCCH but also from CCl2=CFZCCSi(CH3)3.