Abstract: A cyclohexane derivative as shown by formula IB or a stereoisomer or a salt thereof, has a high affinity for D3 receptors and 5-hydroxytryptamine, has a lower affinity for D2 receptors, shows a high selectivity for D3/D2 receptors, and can be used as a therapeutic drug against neuropsychiatric diseases. wherein; X is N or CH; R is R is optionally substituted with one or more substituents selected from the group consisting of F, Cl, Br, I and C1-C6 alkyl; and the C1-C6 alkyl is optionally substituted with one or more substituents selected from the group consisting of F, Cl, Br, and I.
Abstract: Method for preparing cinacalcet hydrochloride having the steps of heating (R)-1-naphthyl ethylamine (Formula I) and 3-(trifluoromethyl)benzene (Formula II) wherein L is a halogen atom, methanesulfonate group (OMs), p-Toluenesulfonate (OTs), or triflate (OTf), in an organic solvent in presence of an inorganic base, refluxing until 3-(trifluoromethyl)benzene is completely consumed, obtaining a reaction mixture containing cinacalcet, and after treatment, obtaining cinacalcet hydrochloride having a formula of The post treatment separates (R)-1-naphthyl ethylamine hydrochloride and cinacalcet hydrochloride by adjusting pH value, extraction, and other simple operations, and the (R)-1-naphthyl ethylamine obtained is recycled for preparing the next batch of cinacalcet hydrochloride.
Abstract: A process for preparation of (1S)-1-phenyl-3,4-dihydro-2(1H)-isoquinoline-carboxylate (Formula I), comprising reacting (1S)-1-phenyl-3,4-dihydro-2(1H)isoquinoline (Formula II) with carbon dioxide and an alkylating agent R-LG in the presence of a base to obtain the compound of Formula I in an organic solvent. In Formula I and II, R is an alkyl or a substituted alkyl; LG is a leaving group.