An efficient and practical synthesis of ropivacaine hydrochloride under ultrasound irradiation

来源 :江苏省药理学会青年工作委员会成立大会暨药理学科青年科技创新学术研讨会 | 被引量 : 0次 | 上传用户:njtangxn
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  Ropivacaine hydrochloride was synthesized from L-2-pipecolic acid by successive reaction with SOCl2 and 2,6-dimethylaniline at 40℃ under ultrasonic irradiation to yield L-N-(2,6-dimethylphenyl)-piperidin-2-carboxamide (4), and 4 was reacted with l-bromopropane at 50℃ for 1 h under ultrasonic irradiation.The effects of reaction solvent, temperature and time under ultrasonic irradiation were investigated.Compared with conventional methods, present procedures have the advantages in milder conditions, shorter reaction time and higher yields.The total yield was 67.5%, [α]2o5=-6.6°(c =2, H2O).
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