Tetrazole derivatives
US-2024382468-A2 · Nov 21, 2024 · US
US12454528B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12454528-B2 |
| Application number | US-202017785828-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 14, 2020 |
| Priority date | Dec 16, 2019 |
| Publication date | Oct 28, 2025 |
| Grant date | Oct 28, 2025 |
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The present invention relates to process for the preparation of a compound of formula (1), wherein R1 and R2 are independently from each other C1-C8alkyl, which comprises reacting a compound of formula (2), with a formaldehyde source in presence of a palladium or platinum catalyst at a hydrogen pressure of 5×108 mPa to 200×108 mPa.
Opening claim text (preview).
The invention claimed is: 1 . A process for the preparation of a compound of formula wherein R 1 and R 2 are independently from each other C 1 -C 8 alkyl, comprising reacting a compound of formula with a formaldehyde source in presence of a palladium or platinum catalyst at a hydrogen pressure of 5×10 8 mPa to 200×10 8 mPa. 2 . The process according to claim 1 , wherein R 1 and R 2 are independently from each other C 1 -C 4 alkyl. 3 . The process according to claim 1 , wherein the formaldehyde source is paraformaldehyde or formaldehyde. 4 . The process according to claim 1 , wherein the process is carried out at a temperature of 50 to 180° C. 5 . The process according to claim 1 , wherein the process is carried out at a temperature of 80 to 150° C. 6 . The process according to claim 1 , wherein a palladium or platinum catalyst supported on a carbon carrier is used. 7 . The process according to claim 1 , wherein a palladium catalyst supported on a carbon carrier is used. 8 . The process according to claim 1 , wherein a platinum catalyst supported on a carbon carrier is used. 9 . The process according to claim 1 , wherein 2 to 15 weight-% of the catalyst is used, based on the weight of the compound of formula (2). 10 . The process according to claim 1 , wherein the reaction is carried out in presence of a solvent. 11 . The process according to claim 10 , wherein the solvent is water, hexane, methanol, toluene or xylene. 12 . A method for the preparation of compounds of formula wherein R 3 is a group of formula comprising reacting compounds of formula (1), according to claim 1 , with a compound of formula NH 2 —(CH 2 ) 3 —NH—(CH 2 ) 2 —NH—(CH 2 ) 3 —NH 2 (6), or for the preparation of compounds of formula and wherein R 1 and R 2 are as defined in claim 1 , and R 4 and R 5 are hydrogen or methyl, comprising reacting compounds of formula (1), according to claim 1 , with a compound of formula wherein R 4 and R 5 are hydrogen or methyl. 13 . The process according to claim 1 , wherein R 1 and R 2 are butyl. 14 . The process according to claim 10 , wherein the solvent is methanol. 15 . The process according to claim 10 , wherein the solvent is toluene. 16 . The process according to claim 10 , wherein the solvent is xylene. 17 . The process according to claim 12 , wherein the reaction is carried out in presence of a solvent. 18 . The process according to claim 17 , wherein the solvent is toluene, xylene or trimethylbenzene.
containing three or more hetero rings · CPC title
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