116753-41-4

Upstream product

• 1359159-58-2 8-(4,4-dimethoxybutyl)-8-azaspiro[4.5]decane-7,9-dione 
• 1075-89-4 tetramethylene glutarimide 
• 110-52-1 1,4-dibromo-butane 
• 20980-22-7 N-(2-pyridinyl)piperazine 
• 94021-22-4 1-(2-pyrimidyl)piperazine dihydrochloride 

Relevant academic research and scientific papers

An efficient synthesis of aripiprazole, buspirone and NAN-190 by the reductive alkylation of amines procedure

The reductive alkylation of amines procedure was applied for the synthesis of aripiprazole 1a, buspirone 1b, and NAN-190 1c. The reductive alkylation of amines procedure was applied for the synthesis of aripiprazole 1a, buspirone 1b, and NAN-190 1c. Copyright

The preparation of 8-[4-[4-(2-pyrimidinyl)-1-piperaziny]butyl]-8- azaspiro[4,5] decane-7,9-dione hydrochloride

8-[4-[4-(2-Pyrimidinyl)-1-piperaziny]butyl]-8-azaspiro [4,5] decane-7,9-dione hydrochloride (buspirone hydrochloride) was obtained in one pot with a 51.8% overall yield. The key intermediate, 1-(2-pyrimidinyl) piperazine, was synthesized through chlorination and cyclization condensation reaction with diethanolamine as initial material. This modified protocol has the notable advantages of mild reaction condition, convenient operation, and high overall yield.

Process for the preparation of high purity buspiron and the hydrochloride thereof

Process for the preparation of 8 -[4 -[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione (buspiron) of the Formula I STR1 and the hydrochlorides thereof having high purity by continuously adding a solution of 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-but-2 -inyl]-8-aza-spiro[4.5]decane-7,9-dione of the formula II STR2 formed with an inert organic solvent having a concentration of at least 40% by weight to a suspension of a hydrogenation catalyst in an inert organic solvent and optionally converting the 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-dione thus obtained into the hydrochloride thereof.

Pharmaceutically useful polymorphic modification of buspirone

Buspirone hydrochloride can exist in two polymorphic forms and the newly discoverd lower melting form, which is thermodynamically favored at pharmaceutically relevant temperatures, offers advantage in manufacture of buspirone pharmaceutical compositions .

Process for buspirone hydrochloride polymorphic crystalline form conversion

A process for conversion of one polymorphic crystalline form of buspirone into its other polymorphic crystalline form.

Spiro-quaternary ammonium halides and N-(2-pyrimidinyl)piperazinylalkylazaspiroalkanedione process

Novel spiro-quaternary ammonium halides are disclosed. The new compounds are particularly valuable as intermediates in preparation of N-(2-pyrimidinyl)piperazinylalkyl derivatives of azaspiroalkanediones such as the psychopharmacologic agent 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione.