- Preparation method of varenicline key intermediate
-
The invention discloses a preparation method of a varenicline key intermediate. A target compound is prepared from indanone by the six steps of halogenation, cyanidation, hydrolysis, closed-loop reaction, reduction and hydrochloride formation. The preparation method has the advantages of easy availability of raw materials, mild reaction conditions, simple process, high yield, low cost, low environmental pollution and good utilization value in industrial production.
- -
-
Paragraph 0114-0122
(2019/04/04)
-
- PROCESS FOR PREPARING VARENICLINE, VARENICLINE INTERMEDIATES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
-
Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting l-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien- 10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the pressence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of l-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2- trifluoro-ethanone.
- -
-
Page/Page column 16
(2010/04/06)
-
- PROCESSES FOR THE PREPARATION OF VARENICLINE AND INTERMEDIATES THEREOF
-
The invention provides an improved process for the preparation and purification of Varenicline and intermediates for the preparation of Varenicline.
- -
-
Page/Page column 9
(2009/12/28)
-