Abstract: ABSTRACT AN IMPROVED PROCESS FOR THE PREPARATION OF BUSPIRONE HYDROCHLORIDE The present invention relates to an improved process for the preparation of Buspirone hydrochloride particularly useful in large scale production.
We claim:
1. A process for the preparation of Buspirone or its pharmaceutical^ acceptable salts
comprising the steps of:
(i) reacting 1-(2-pyrimidinyl)-piperazine with 1,4-dibromobutane in the presence of organic base in a suitable solvent to obtain 8-(2-pyrimidinyl)-8-aza-5-azoniaspiro[4,5]decane bromide; (ii) reacting the obtained 8-(2-pyhmidinyl)-8-aza-5-azoniaspiro[4,5]decane bromide with 3,3-tetramethylene glutarimide in the presence of potassium-t-butoxide in n-butyl acetate to obtain Buspirone free base; and (iii) treating the Buspirone free base with hydrochloric acid in ethyl acetate to obtain Buspirone hydrochloric acid.
2. The process for the preparation of Buspirone or its pharmaceutical^ acceptable salts according to claim-1, wherein the said organic base is triethylamine.
3. The process for the preparation of Buspirone or its pharmaceutically acceptable salts according to claim-1, wherein the suitable solvent is selected from the group consisting of alcohols, ethers, esters, ketones, nitriles, amides, sulfoxides, aliphatic and aromatic hydrocarbons, halogenated hydrocarbons, and mixtures of two or more thereof.
4. A process for the preparation of Buspirone or its pharmaceutically acceptable salts comprising the steps of:
(i) reacting 1-(2-pyrimidinyl)-piperazine with dibromobutane in the presence of
organic base in a suitable solvent to obtain 8-(2-pyrimidinyl)-8-aza-5-
azoniaspiro[4,5]decane bromide; (ii) reacting the obtained 8-(2-pyrimidinyl)-8-aza-5-azoniaspiro[4,5]decane bromide
with 3,3-tetramethylene glutarimide in the potassium-t-butoxide in n-butyl acetate
to obtain Buspirone free base; and (iii) optionally treating the Buspirone free base with an acid in an organic solvent to
obtain corresponding pharmaceutically acceptable salt of Buspirone.
5. The process for the preparation of Buspirone or its pharmaceutical^ acceptable salts according to claim-4, said organic base is triethylamine.
6. The process for the preparation of Buspirone or its pharmaceutical^ acceptable salts according to claim-4, wherein the suitable solvent is selected from the group consisting of alcohols, ethers, esters, ketones, nitriles, amides, sulfoxides, aliphatic and aromatic hydrocarbons, halogenated hydrocarbons, and mixtures of two or more thereof.
7. A process for the preparation of Buspirone hydrochloride from Buspirone free base
comprising the step of treating the Buspirone free base with hydrochloric acid in ethyl
acetate.
| # | Name | Date |
|---|---|---|
| 1 | 201941032322-FER.pdf | 2023-06-01 |
| 1 | Form2 Title Page_Complete_09-08-2019.pdf | 2019-08-09 |
| 2 | Form 5_As Filed_09-08-2019.pdf | 2019-08-09 |
| 2 | 201941032322-FORM 18 [12-05-2022(online)].pdf | 2022-05-12 |
| 3 | Form 3_As Filed_09-08-2019.pdf | 2019-08-09 |
| 3 | 201941032322-AMENDED DOCUMENTS [05-04-2021(online)].pdf | 2021-04-05 |
| 4 | 201941032322-FORM 13 [05-04-2021(online)].pdf | 2021-04-05 |
| 4 | Form 1_As Filed_09-08-2019.pdf | 2019-08-09 |
| 5 | Description Complete_As Filed_09-08-2019.pdf | 2019-08-09 |
| 5 | 201941032322-FORM-26 [05-04-2021(online)].pdf | 2021-04-05 |
| 6 | Correspondence by Applicant_As Filed_09-08-2019.pdf | 2019-08-09 |
| 6 | 201941032322-POA [05-04-2021(online)].pdf | 2021-04-05 |
| 7 | Claims_As Filed_09-08-2019.pdf | 2019-08-09 |
| 7 | Abstract_As Filed_09-08-2019.pdf | 2019-08-09 |
| 8 | Claims_As Filed_09-08-2019.pdf | 2019-08-09 |
| 8 | Abstract_As Filed_09-08-2019.pdf | 2019-08-09 |
| 9 | Correspondence by Applicant_As Filed_09-08-2019.pdf | 2019-08-09 |
| 9 | 201941032322-POA [05-04-2021(online)].pdf | 2021-04-05 |
| 10 | 201941032322-FORM-26 [05-04-2021(online)].pdf | 2021-04-05 |
| 10 | Description Complete_As Filed_09-08-2019.pdf | 2019-08-09 |
| 11 | 201941032322-FORM 13 [05-04-2021(online)].pdf | 2021-04-05 |
| 11 | Form 1_As Filed_09-08-2019.pdf | 2019-08-09 |
| 12 | Form 3_As Filed_09-08-2019.pdf | 2019-08-09 |
| 12 | 201941032322-AMENDED DOCUMENTS [05-04-2021(online)].pdf | 2021-04-05 |
| 13 | Form 5_As Filed_09-08-2019.pdf | 2019-08-09 |
| 13 | 201941032322-FORM 18 [12-05-2022(online)].pdf | 2022-05-12 |
| 14 | Form2 Title Page_Complete_09-08-2019.pdf | 2019-08-09 |
| 14 | 201941032322-FER.pdf | 2023-06-01 |
| 1 | SearchStrategyE_23-05-2023.pdf |