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L-Deprenyl hydrochloride, Selegiline hydrochloride, FPF-1100, E-250(free base), Zydis selegilline, Deprenyl, Vivapryl, Zelapar, FP, Plurimen, Seledat, Eldepryl, Jumex

盐酸司来吉兰 司来吉兰 盐酸盐 Chemical Name: (-)-(R)-N,alpha-Dimethyl-N-(2-propynyl)phenethylamine hydrochloride
CAS No. 14611-52-0, 14611-51-9 (free base)
项目整合开发状态: Launched-1981
项目研究机构: Chiesi (Originator), Chinoin (Originator), Schering-Plough (Not Determined), Amarin (Licensee), Asta Medica (Licensee), Elan (Licensee), Fujimoto (Licensee), Orion Pharma (Licensee), Sarget (Licensee), Somerset (Licensee), Valeant (Licensee)
合成路线:Compound can be prepared in several related ways:1) The condensation of N-(1-phenylisopropyl)methylamine (I) with 1,2-dibromopropene (A) by heating at 100 C gives N-(1-phenylisopropyl)-N-methyl-2-bromopropenylamine (II),which is then dehydrobrominated and isomerized by treating with KOH in refluxing ethanol water.2) By heating a mixture of (I) and propargyl bromide (B) at 100 C.3) By reductocondensation of (I) with propargyl aldehyde (C) by means of amalgamated Al in ethanol.4) By condensation of (I) with formaldehyde and acetylene by means of CuCl in hot dioxane.5) By condensation of 1-phenylisopropyl chloride (III) with N-methylpropargylamine (IV) by heating at 80 C in a sealed tube.
📌 参考资料/链接:
参考文献标题:Selegiline
文献作者:Roberts,P.J.; Castar,J.
参考来源:Drugs Fut 1979,4(2),128

📄 详细内容


合成路线:The reduction of 11C-CO2 (I) by means of LiAlH4 in THF gives 11C-methanol (II),which is treated with 57 % IH to yield 11C-methyl iodide (III).The reaction of (III) with silver triflate affords 11C-methyl triflate (IV).Finally,(R)(-)-nor-selegiline (nor-deprenil) (V) is methylated with the radiolabeled methyl triflate (IV) by means of NaOH in aqueous acetone to obtain the target radiolabeled compound.

参考文献标题:Efficient synthesis and formulation of (R)-(-)-[11C]deprenyl,a selective radioligand for the quantification of MAO-B activity using PET
文献作者:Dolle,F.; et al.
参考来源:J Label Compd Radiopharm 2002,45(10),803


合成路线:Compound can be prepared in several related ways:1) The condensation of N-(1-phenylisopropyl)methylamine (I) with 1,2-dibromopropene (A) by heating at 100 C gives N-(1-phenylisopropyl)-N-methyl-2-bromopropenylamine (II),which is then dehydrobrominated and isomerized by treating with KOH in refluxing ethanol water.2) By heating a mixture of (I) and propargyl bromide (B) at 100 C.3) By reductocondensation of (I) with propargyl aldehyde (C) by means of amalgamated Al in ethanol.4) By condensation of (I) with formaldehyde and acetylene by means of CuCl in hot dioxane.5) By condensation of 1-phenylisopropyl chloride (III) with N-methylpropargylamine (IV) by heating at 80 C in a sealed tube.

参考文献标题:Verfahren zur Herstellung von Phenylisopropylaminen
文献作者:Ecsery,Z.; et al.
参考来源:CH 530953; DE 1227447


合成路线:Compound can be prepared in several related ways:1) The condensation of N-(1-phenylisopropyl)methylamine (I) with 1,2-dibromopropene (A) by heating at 100 C gives N-(1-phenylisopropyl)-N-methyl-2-bromopropenylamine (II),which is then dehydrobrominated and isomerized by treating with KOH in refluxing ethanol water.2) By heating a mixture of (I) and propargyl bromide (B) at 100 C.3) By reductocondensation of (I) with propargyl aldehyde (C) by means of amalgamated Al in ethanol.4) By condensation of (I) with formaldehyde and acetylene by means of CuCl in hot dioxane.5) By condensation of 1-phenylisopropyl chloride (III) with N-methylpropargylamine (IV) by heating at 80 C in a sealed tube.

参考文献标题:Verfahren zur Herstellung von Phenylisopropylaminen
文献作者:Ecsery,Z.; et al.
参考来源:DE 1568277; NL 6605956


合成路线:Compound can be prepared in several related ways:1) The condensation of N-(1-phenylisopropyl)methylamine (I) with 1,2-dibromopropene (A) by heating at 100 C gives N-(1-phenylisopropyl)-N-methyl-2-bromopropenylamine (II),which is then dehydrobrominated and isomerized by treating with KOH in refluxing ethanol water.2) By heating a mixture of (I) and propargyl bromide (B) at 100 C.3) By reductocondensation of (I) with propargyl aldehyde (C) by means of amalgamated Al in ethanol.4) By condensation of (I) with formaldehyde and acetylene by means of CuCl in hot dioxane.5) By condensation of 1-phenylisopropyl chloride (III) with N-methylpropargylamine (IV) by heating at 80 C in a sealed tube.

参考文献标题:
文献作者:Ecsery,Z.; et al.
参考来源:AT 251560


合成路线:Compound can be prepared in several related ways:1) The condensation of N-(1-phenylisopropyl)methylamine (I) with 1,2-dibromopropene (A) by heating at 100 C gives N-(1-phenylisopropyl)-N-methyl-2-bromopropenylamine (II),which is then dehydrobrominated and isomerized by treating with KOH in refluxing ethanol water.2) By heating a mixture of (I) and propargyl bromide (B) at 100 C.3) By reductocondensation of (I) with propargyl aldehyde (C) by means of amalgamated Al in ethanol.4) By condensation of (I) with formaldehyde and acetylene by means of CuCl in hot dioxane.5) By condensation of 1-phenylisopropyl chloride (III) with N-methylpropargylamine (IV) by heating at 80 C in a sealed tube.
参考文献标题:
文献作者:Ecsery,Z.; et al.
参考来源:AT 252901


产品链接: CAS No. 14611-52-0››

产品链接: CAS No.14611-51-9››