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Two methods for the preparation of 5-iodo-1,2,3-triazolyl-4-phosphonate were explored. This compound was then functionalized by Suzuki and Stille cross-coupling reaction to obtain 5-aryl-, 5-heteroaryl- or 5-alkenyl-1,2,3-triazolyl-4-phosphonates. 5-Iodo-1,2,3-triazolyl-4-phosphonate is prepared from diethyl ethynylphosphonate by one-pot regioselective 1,3-dipolar cycloaddition/iodation reaction and used in Suzuki and Stille cross-coupling reactions.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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This study presents the first example of the Pd-catalyzed cascade reactions of 5-oxohexanenitrile with arylboronic acids, affording important synthon 2-methylpyridines that can be further translated through C(sp3)-H functionalization to construct pyridine derivatives. Furthermore, this chemistry allows 5-oxo-5-Arylpentanenitrile to react with arylboronic acids to provide unsymmetrical 2,6-diarylpyridines. This protocol paves the way for the practical and atom economical syntheses of valuable pyridines with broad functional groups in moderate to excellent yields under mild conditions.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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A substituted tricyclohexylphosphane with ?conformational lock?, tri(4-trans-(tert-butyl)cyclohexyl)phosphane L, has been designed and synthesized. The ligand has shown similar steric bulkiness and conformations to tricyclohexylphosphane at solid state. The comparable or slightly better performance of ligand L compared to PCy3 in Suzuki-Miyaura coupling has demonstrated the similar steric properties of two ligands in reaction and the effectiveness of the chair conformer of the cyclohexyl rings. The ineffectiveness of both L and PCy3 in palladium-catalyzed aminations has also manifested the weakness of such ligands and a sterically more bulky ligand is needed in order to develop a more efficient amination.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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5-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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The base-free palladium-catalyzed borylation of aryl chlorides with diborons was achieved. The base-free conditions offered acceptable functional group compatibility. Based on experimental and computational studies, it was shown that smooth boryl transfer from the diborons to the arylpalladium chloride was promoted by strong interaction between the Lewis acidic boron and the chlorine atom on palladium.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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An efficient and stereoselective synthesis of pyrrolidine-, piperidine-, and azepane-type N-heterocycles is described by the intramolecular Pd(0)-catalysed cyclisation of amino allylic carbonates. The use of chiral ligands gave the corresponding heterocyclic derivatives having er values that were from moderate to good.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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9 – (Arylamino) – 9H – efficient production of aryl [to] carbazole. [Solution] a palladium compound, a phosphine compound, in the presence of a metal alkoxide, (1) represented by the formula […], carbazole derivative of the reaction. (Ar each independently a phenylene group or the like, the number of 1 – 4 carbon alkyl group substituted phenylene group or the like or may be; X is independently Cl, Br or I; 1 or 2 respectively and independently p q; R1 Are each independently a C1 a-6 alkyl group, a phenyl group, naphthyl group, pyridyl group or biphenylyl group; m is 1 or 2; n is 0 or 1; m + n=2)[Drawing] no (by machine translation)

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Substituted phenanthrene-9,10-diones in accord with structural diagram I, 1compositions thereof and methods for the use thereof, for the treatment of T cell mediated conditions such as autoimmune diseases and organ graft rejection. In compounds of the invention, R1 at each occurrence is independently selected from hydrogen, halogen, NH-tosyl, N-di-tosyl, NH2, NO2, NH?CO?R2, CO?NH?R2, Ar, (CH2)nCH(COOH)R3 COR3 and NHCOCH2CH(COOH)NHR4, where R2, R3 and R4 are a selected from a variety of substituted or unsubstituted alkyl and aryl groupstand oligopeptides.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method