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 1-(45-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7)35-trien-10-yl)-222-trifluoro-ethanone with chloroacetaldehyde in the presence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of 1-(45-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-...

Crystalline forms of Varenicline Tosylate processes for preparing those crystalline forms of Varenicline Tosylate and processes for obtaining high purity Varenicline base using Varenicline Tosylate are provided.

Provided herein is an impurity of varenicline, 6-methyl-5,8,14-triazatetracyclo[l 0.3.1.02'n,04'9]hexadeca-2(l l),3,5,7,9-pentaene (methylvarenicline) impurity, and a process for the preparation and isolation thereof. Provided further herein is a highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity, a process for the preparation thereof, and pharmaceutical compositions comprising highly pure varenicline or a pharmaceutically accep...

Salts and crystalline forms of several salts of Varenicline i.e. Varenicline sulfate: are provided along with methods of preparing the solid states and processes for preparing Varenicline base from those Varenicline salts.

Disclosed herein is a stable amorphous coprecipitate comprising varenicline tartrate and a pharmaceutically acceptable excipient selected from the group consisting of maltodextrin lactose monohydrate and 2-hydroxypropyl-&bgr;-cyclodextrin method for the preparation pharmaceutical compositions and method of treating thereof. Advantageously the amorphous coprecipitates of varenicline tartrate disclosed herein have improved physiochemical characteristics that assist in the effective bioavailability...

Disclosed herein is a stable amorphous coprecipitate comprising varenicline tartrate and a pharmaceutically acceptable excipient selected from the group consisting of maltodextrin, lactose monohydrate and 2-hydroxypropyl-[beta]-cyclodextrin, method for the preparation, pharmaceutical compositions, and method of treating thereof. Advantageously, the amorphous coprecipitates of varenicline tartrate disclosed herein have improved physiochemical characteristics that assist in the effective bioavaila...