SEPARATION OF ENANTIOMERS OF 3-ETHYLBICYCLO[3.2.0]HEPT-3-EN-6-ONE

• Main Authors: FORD RHONAN LEE, MEGHANI PREMJI
• Format: Patent
• Language: Chinese; English
• Published: 06.02.2018
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; APPARATUS THEREFOR; CHEMISTRY; GENERAL METHODS OF ORGANIC CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention relates to a process to isolate a compound of Formula (2a) or a salt or solvate thereof, comprising a) reacting a mixture of diastereoisomers of Formulae (2a, 2b) with a basic heterocyclic-aldehyde compound and an optically active amine in the presence of a base; and b) separating the compound of Formula (2a) from the product of step a) by acid extraction. The compound of Formula (2a) may be produced with an enantiomeric excess of 98%. Compounds of Formula (2a) are useful intermediates in a process to prepare a bicyclic gamma - amino tetrazole derivative of Formula (I) which finds utility in treating neuropathic pain and disorders of the central nervous system. 本发明涉及种分离式(2a)的化合物或其盐或其溶剂化物的方法，包括：a)使式(2a，2b)的非对映异构体的混合物与碱性杂环-醛化合物和光学活性胺在碱存在下反应；和b)通过酸提取从步骤a)的产物中分离式(2a)的化合物。式(2a)化合物可以以98％的对映体过量产生。式(2a)化合物在制备式(I)的双环γ-氨基四唑衍生物的方法中是有用的中间体，其用于治疗神经性疼痛和中枢神经系统失调。