The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Mitotic kinesin inhibitors

Bicyclic Conformationally Restricted Diamines

The preparation methods and reactions of isoxazoles are described and systematized on the basis of analysis of the literature published from 2005 to present. In the discussion of synthesis, major attention is focused on the most efficient approaches: condensation of hydroxylamine with 1,3-dielectrophiles and reactions of nitrile oxides with alkenes and alkynes. Five-membered ring opening reactions leading to acyclic functionalized or other heterocyclic compounds are considered. The transformations of isoxazole derivatives that occur without ring cleavage to form fused heterocyclic systems, as well as reactions that lead to the introduction of C-substituents into isoxazoles, are considered. Data on the biological activity of some isoxazole derivatives are reported. The bibliography includes 439 references.

http://iopscience.iop.org/article/10.1070/RCR4503/pdf

Recent advances in isoxazole chemistry

The 1,3-dipolar cycloaddition reaction of nitrile oxides with carbon dipolarophiles is a versatile and powerful synthetic method to prepare isoxazolines. In particular nitrile oxide cycloaddition reactions with exocyclic methylene or alkylidene compounds generally proceed regioselectively leading to spiro heterocyclic compounds. This review deals with progress in the field of nitrile oxide cycloaddi- tion chemistry for the synthesis of spiro isoxazolines.

Spiro Isoxazolines via Nitrile Oxide 1,3-Dipolar Cycloaddition Reactions

The α-keto methylene group in 3,5-diaryl-2-cyclohexenones 2 and 3,5-diarylcyclohexanones 8 have been used to obtain fused pyrazoles and isoxazoles. The new compounds were characterized by IR and 1H-NMR spectral data.

/pdf/synthesis-of-some-fused-pyrazoles-and-isoxazoles-1aumxyuf8v.pdf

Synthesis of Some Fused Pyrazoles and Isoxazoles

Cyclohexenone carboxylates. a versatile source for fused isoxazoles and pyrazoles

The reaction of semicarbazones of 3,5-diphenylcyclohex-2-enone 2 and 3,5-diphenylcyclohexanone 8 with selenium dioxide and thionyl chloride resulted in annelated 1,2,3-selena- and thia-diazoles 3, 4, 5, 9 and 10.

Synthesis of Annelated 1,2,3-Selena- or -Thia-diazoles

1,3-Dipolar Cycloaddition of Dipolar Reagents to Bifunctional Olefins with Chloramine-T --- Part-II

1,4-pentadien-3-ones. a source for selenano 1,2,3- selena and thiadiazoles

The reactivity of 3,5-di ary1 cyclohexanone 1 lead to th e formation of a vari ety of spiro cyclohexanes viz. cyclohexanooxirane 2, cyclohexanocyclopropane 4, cyclohexanothiirane 5 and cyclohexanoaziridine 6. In recent past we have been actively engaged In expl oi ting th e a -keto methylene functionality of homolheterocyclic ketones in the development of I ,2,3-selena/thiadiazoles, 1-4 isoxazolines/pyrazolines 5 , triazol es 6 etc. In view of our successful results on thi s front, the reactivity of 3,5-diaryl-2-cyclohexane was further studied . The in-built spiro carbocyclic or heterocyclic systems in a ring generally increases the biological potency more so with systems havi ng small er rings. In fact, hetero atoms in small rings affect bond angles, bond lengths and bond strengths through a combination of factors including their intrinsic hybridi zation, magnitude of covalent radii , angle bending constants, non-bonded interactions and long range electronic effects. The present study, therefore, aims at the development of hitherto unknown[3,6] rin g systems. The 3,5-diphenylcyclohexanone 1 was obtained fro m the decarboxylation and catalytic hydrogenati on of 6-carbethoxy-3,5-diphenylcyclohexenone, which in turn was prepared by Knoevenagel reaction of ethyl acetoacetate and 1,3 -di aryl-2-propen-l-one in the presence of sodium ethoxide 7 . The cycloaddition of dimethylsulfoxonium methylide 8 • 9 . lo which is generated in situ from trimethylsulfoxonium iodide (TMSOI) to 1 in presence of KBuO t

/pdf/reactivity-of-3-5-diaryl-cyclohexanones-synthesis-of-spiro-4kceevaazx.pdf

Reactivity of 3,5-diaryl cyclohexanones - Synthesis of spiro cyclohexanes

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