Varenicline tartrate synthesis

Yield:375815-87-5 84%

Reaction Conditions:

in methanol

Steps:

1 Comparative Example 1 Preparation of Barrenicin L-tartarate
16.5 g (0.11 mol) of L-tartaric acidIt is dissolved in 158 mL of methyl alcohol and filtered.To the filtrate was added 21.1 g (0.10 mole) of7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino [2,3-h] [3]Dissolve in 158 mL of methyl alcohol for 45 minutes.The resulting crystals were stirred overnight, filtered under reduced pressure, and vacuum-dried at 35 to 45 ° C to obtain 30.2 g (84%) of Barrenicin L-tartarate.

References:

KyungDong Pharmaceutical Company;Lee Byeong-seok;Kil Hyeong-jun;Shin Sang-hun;Lee Gi-yeong;Song U-ryul KR101781352, 2017, B1 Location in patent:Paragraph 0100-0101

FullText