Sign In to Follow Application
View All Documents & Correspondence

An Improved Process For The Preparation Of Buspirone Hydrochloride

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.

Get Free WhatsApp Updates!
Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
09 August 2019
Publication Number
07/2021
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
afzal@hasanandsingh.com
Parent Application

Applicants

Solara Active Pharma Sciences Limited
SAPS Research Centre, 27, Vandaloor Kelambakkam Road, Keelakottaiyur Village, Melakottaiyur Post, Chennai-600127, Tamil Nadu, India.

Inventors

1. HOLKAR, Anil Ganpatrao
Dr. Anil Ganpatrao Holkar, #23, Saikrupa, 1st Cross MMG Gardenia, Somanath Nagar, Dattagalli 3rd Stage, Mysore, Karnataka-570022, India.
2. TIMMANAGOUDA, Karabasanagouda
Sri Mallikarjuna D. No; 1-184/C18, Deepa Farm Road, Shivagiri Nagara Kulai-Hosabettu, Mangalore, Karnataka-575019 , India.
3. MOHANAKRISHNAN, Jeyakumar
Plot No: 13, Sakthi nagar, 15Th street, Nerkundram, Chennai- 600107, Tamil Nadu, India.
4. CHANDIRASEKAR, Manlckam
2/96, periyandipatti, kanderkulamanickam post, Sankiri taluk, Salem, Tamil Nadu, India- 637501
5. SRINIVASAN, Swaminathan
3E, Classic Rudra Ramaniyam Apts, 3rd East Street, Kamaraj Nagar, Thiruvanmiyur, Chennai- 600041, Tamil Nadu, India.

Specification

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.

Documents

Application Documents

# 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

Search Strategy

1 SearchStrategyE_23-05-2023.pdf