The present invention relates to a Palladium (II)-catalyzed C(sp.sup.3)H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs.

The present invention relates to a Palladium (II)-catalyzed C(sp.sup.3)H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs.

There is a demand for the development of a technique according to which a reaction for coupling a halogenated pyridine compound with a halogenated aromatic compound can be performed in a simple manner through a small number of steps without using expensive agents such as a palladium catalyst. A method for coupling a halogenated pyridine compound with a halogenated aromatic compound includes a step of coupling a halogenated pyridine compound with a halogenated aromatic compound to obtain a pyridine compound by reacting, in a reaction solvent, the halogenated pyridine compound and the halogenated aromatic compound with a solution containing an alkali metal.

There is a demand for the development of a technique according to which a reaction for coupling a halogenated pyridine compound with a halogenated aromatic compound can be performed in a simple manner through a small number of steps without using expensive agents such as a palladium catalyst. A method for coupling a halogenated pyridine compound with a halogenated aromatic compound includes a step of coupling a halogenated pyridine compound with a halogenated aromatic compound to obtain a pyridine compound by reacting, in a reaction solvent, the halogenated pyridine compound and the halogenated aromatic compound with a solution containing an alkali metal.

The present invention relates to a Palladium (II)-catalyzed C(sp.sup.3)-H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs.

The present invention relates to a Palladium (II)-catalyzed C(sp.sup.3)-H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs.

The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I) ##STR00001##
wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I) ##STR00001##
wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

The present invention discloses a cobalt compound of formula (I), a process for the preparation and use thereof. The present invention further relates to a pharmaceutical composition and a method inhibition of Tau Aggregation in a subject in need thereof using compound of formula (I).

##STR00001##

The present invention provides a palladium(II) complex of formula (1) or a palladium(II) complex of formula (2).

##STR00001##

R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.18, R.sub.19, R.sub.20, R.sub.21, R.sub.22, R.sub.23 and R.sub.24, m, E and X are described in the specification. The invention also provides a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.