Base metal catalyzed borylation of arenes and aromatic heterocycles
US-2016318963-A1 · Nov 3, 2016 · US
US11040994B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11040994-B2 |
| Application number | US-201816620125-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 6, 2018 |
| Priority date | Jun 6, 2017 |
| Publication date | Jun 22, 2021 |
| Grant date | Jun 22, 2021 |
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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).
Opening claim text (preview).
We claim: 1. A cobalt complex compound selected from a group consisting of Cobalt(II)(2,6-bis((4-methylpiperazin-1-yl)methyl)pyridine) chloride 1A), Cobalt(II)(2,6-bis(piperazin-1-ylmethyl)-pyridine) chloride (IB), Cobalt(II)(2,6-bis(morpholinomethy)pyridine) chloride (1C), Cobalt(II)(2,6-bis(piperidin-1-ylmethyl)pyridine) chloride (ID), Cobalt(II)(2,6-bis((4-methylpiperazin-1 yl)methyl)pyridine) bromide (2A), Cobalt(II)(2,6-bis(piperazin-1-ylmethyl)pyridine) bromide (2B), Cobalt(II)(2,6-bis(morpholinomethyl)pyridine) bromide (2C), and Cobalt(II)(2,6-bis(piperidin-1-ylmethyl)pyridine)bromide (2D). 2. A process for synthesis of cobalt complex compounds each as claimed in claim 1 , comprising the steps of: a) adding a solution of 2,6-bis(bromomethyl)pyridine in acetonitrile to a solution of an amine and a baser in solvent followed by stirring at a temperature in the range of 80 to 90° C. for a period in the range of 14 to 16 hours to afford NNN-Ligand; b) adding a solution of Cobalt halo hexahydrate in solvent to a solution of NNN-Ligand of step (a) in solvent with stirring for 3 to 4 hours at a temperature range of 25 to 30° C. to afford the desired cobalt complex compounds. 3. The process as claimed in claim 2 , wherein said base is selected from the group consisting of potassium carbonate, sodium carbonate, lithium carbonate, caesium carbonate, sodium hydride, cesium fluoride, tripotasium phosphate, monopotassium phosphate or potassium bicarbonate. 4. The process as claimed in claim 2 , wherein said amine is selected from the group consisting of morpholine, piperidine 1-methylpiperazine, and piperazine. 5. The process as claimed in claim 2 , wherein said solvent is selected from the group consisting of methanol, acetonitrile, ethanol, dimethylformamide, dimethyl sulfoxide, isopropyl alcohol or tetrahydrofuran. 6. A pharmaceutical composition comprising the compound according to claim 1 , or a stereoisomer, or ester or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, diluent or excipient. 7. A method for inhibiting Tau aggregation in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of the cobalt complex compound according to claim 1 , or a pharmaceutically acceptable salt thereof. 8. A process for selective hydrogenation of alkenes or alkynes in the presence of the cobalt complex compound according to claim 1 , as catalysts, the process comprising mixing alkyne/alkene, amino-borane, the cobalt complex compound and methanol, followed by stirring for a period in the range of 10 to 14 h at a temperature range of 50 to 80° C. to obtain the desired alkene/alkane. 9. The process as claimed in claim 8 , wherein said alkyne/alkene is an alkyne selected from the group consisting of internal alkyne or terminal alkyne, or is a terminal alkene; and said cobalt complex compound is selected from compounds 1A, 1B, 1C, 1D, 2A, 2B, 2C or 2D.
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