【药物名称】Delergotrile, CM-29712
化学结构式(Chemical Structure):
参考文献No.900348
标题:
作者:Stuetz, P.; et al.
来源:BE 831488; CH 605936; CH 605938; DE 2530577; FR 2282889; GB 1517971; GB 1517972; GB 1517973; JP 7634199; JP 7783598; NL 7508416; ZA 7504642
合成路线图解说明:

This compound can be obtained in two related ways: 1) The dehydrogenation of methyl 9,10-dihydrolysergate (I) with MCPBA and triethylamine in dichloromethane gives methyl ergolene-8-carboxylate (II), which is hydrogenated with H2 over PtO2 in DMF - acetic acid yielding methyl 9,10-dihydroisolysergate (III). The reduction of (III) with LiAlH4 as usual affords 9,10-dihydroisolysergol-(6-methyl-8-hydroxymethylergoline) (IV), which by reaction with methanesulfonyl chloride in acetonitrile yields the corresponding mesylate (V). Finally this compound is treated with KCN in hot DMF - water(1,2). 2) Compound (IV) is treated with refluxing POCl3 to give 6-methyl-8-chloromethylergolin (VI), which is finally treated with NaCN in DMSO at 120 C (3).

参考文献No.950095
标题:Ergot alkaloids. New ergolines as selective dopaminergic stimulants
作者:Stuetz, P.; et al.
来源:J Med Chem 1978,21754-757
合成路线图解说明:

This compound can be obtained in two related ways: 1) The dehydrogenation of methyl 9,10-dihydrolysergate (I) with MCPBA and triethylamine in dichloromethane gives methyl ergolene-8-carboxylate (II), which is hydrogenated with H2 over PtO2 in DMF - acetic acid yielding methyl 9,10-dihydroisolysergate (III). The reduction of (III) with LiAlH4 as usual affords 9,10-dihydroisolysergol-(6-methyl-8-hydroxymethylergoline) (IV), which by reaction with methanesulfonyl chloride in acetonitrile yields the corresponding mesylate (V). Finally this compound is treated with KCN in hot DMF - water(1,2). 2) Compound (IV) is treated with refluxing POCl3 to give 6-methyl-8-chloromethylergolin (VI), which is finally treated with NaCN in DMSO at 120 C (3).

参考文献No.950096
标题:Synthesis of nitrile and amide of D-6-methyl-8-isoergolin-I-ylacetic acid and of nitrile of D-isoergolin -II-yl-acetic acid
作者:Zik醤, V.; et al.
来源:Coll Czech Chem Commun 1976,41(9),2761-2764
合成路线图解说明:

This compound can be obtained in two related ways: 1) The dehydrogenation of methyl 9,10-dihydrolysergate (I) with MCPBA and triethylamine in dichloromethane gives methyl ergolene-8-carboxylate (II), which is hydrogenated with H2 over PtO2 in DMF - acetic acid yielding methyl 9,10-dihydroisolysergate (III). The reduction of (III) with LiAlH4 as usual affords 9,10-dihydroisolysergol-(6-methyl-8-hydroxymethylergoline) (IV), which by reaction with methanesulfonyl chloride in acetonitrile yields the corresponding mesylate (V). Finally this compound is treated with KCN in hot DMF - water(1,2). 2) Compound (IV) is treated with refluxing POCl3 to give 6-methyl-8-chloromethylergolin (VI), which is finally treated with NaCN in DMSO at 120 C (3).

参考文献No.950097
标题:Delergotrile
作者:Blancafort, P.; Serradell, M.N.; Casta馿r, J.; Paton, D.M.
来源:Drugs Fut 1980,5(10),485
合成路线图解说明:

This compound can be obtained in two related ways: 1) The dehydrogenation of methyl 9,10-dihydrolysergate (I) with MCPBA and triethylamine in dichloromethane gives methyl ergolene-8-carboxylate (II), which is hydrogenated with H2 over PtO2 in DMF - acetic acid yielding methyl 9,10-dihydroisolysergate (III). The reduction of (III) with LiAlH4 as usual affords 9,10-dihydroisolysergol-(6-methyl-8-hydroxymethylergoline) (IV), which by reaction with methanesulfonyl chloride in acetonitrile yields the corresponding mesylate (V). Finally this compound is treated with KCN in hot DMF - water(1,2). 2) Compound (IV) is treated with refluxing POCl3 to give 6-methyl-8-chloromethylergolin (VI), which is finally treated with NaCN in DMSO at 120 C (3).

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