首页> 外国专利> analogifremgangsmåde to manufacture (4ars, 5sr, 9bsr) - or (4ars, 5sr, 9brs) - 1,3,4,4a, 5,9b - hexahydro-3,6-dimethyl-2 - 5 - phenyl - 2h indeno 1,2 - c production.

analogifremgangsmåde to manufacture (4ars, 5sr, 9bsr) - or (4ars, 5sr, 9brs) - 1,3,4,4a, 5,9b - hexahydro-3,6-dimethyl-2 - 5 - phenyl - 2h indeno 1,2 - c production.

机译:Analogifremgangsmåde生产(4ars,5sr,9bsr)-或(4ars,5sr,9brsr)-1,3,4,4a,5,9b-六氢-3,6-二甲基-2-5-苯基-2h茚并[1 ,2-c]生产。

摘要

Preparation of new (4aRS,5SR,9bSR)- and (4aRS,5SR,9bRS)-1,3,4,4a,5,9b-hexahydro-5-phenyl-2H-indeno 1,2,c - pyridines of formula (I) is effected by the following schemes: (R1=R11=lower alkyl, alkenyl or alkynyl) X = acid residue of a reactive ester cyclising to I cyclising with polyphosphoric acid to I (R1II=R1=H, lower alkyl or alkenyl; R3=R2) reduction with lithium aluminium hydride right arrow I (R1=H or lower alkyl) aluminium hydride or diborane Ie (R1 = H, lower alkyl or alkoxy) (hydrogenolytic) right arrow I (R1 = H) splitting (R4 = methyl or benzyl) or heating a cpd. (4aRS,5SR,9bRS) of formula (I) in alkaline medium to obtain a cpd. (4aRS,5RS,9bRS) of formula (I) and desirably separating the mixture of (4aRS,5SR,9bSR) and (4aRS,5SR,9bRS) cpds. into their isomers. In the formulae either R1, R2 and R3 stand for H or R1 is H, lower alkyl, alkenyl or alkynyl or has a limited meaning as given in brackets uner specific formulae, R2 is Cl, Br, F or lower alkyl and R3 is H, Cl, Br, F or a lower alkyl, alkylthio- or alkoxy gp. or trifluoromethyl.
机译:制备新的(4aRS,5SR,9bSR)-和(4aRS,5SR,9bRS)-1,3,4,4a,5,9b-六氢-5-苯基-2H-茚满1,2,c-式吡啶(I)通过以下方案实现:(R1 = R11 =低级烷基,烯基或炔基)X =反应性酯的酸残基环化成I,用多磷酸环化成I(R1II = R1 = H,低级烷基或烯基) ; R3 = R2)用氢化铝锂还原右箭头I(R1 = H或低级烷基)氢化铝或乙硼烷Ie(R1 = H,低级烷基或烷氧基)(氢解)右箭头I(R1 = H)拆分(R4 =甲基或苄基)或加热cpd。在碱性介质中将式(I)的化合物(4aRS,5SR,9bRS)获得cpd。式(I)的(4aRS,5RS,9bRS)和期望地分离(4aRS,5SR,9bSR)和(4aRS,5SR,9bRS)cpds的混合物。进入他们的异构体。在式中,R 1,R 2和R 3代表H,或R 1是H,低级烷基,烯基或炔基或在括号中具有特定含义的特定含义,R 2是Cl,Br,F或低级烷基,R 3是H ,Cl,Br,F或低级烷基,烷硫基或烷氧基gp。或三氟甲基。

著录项

  • 公开/公告号DK130292B

    专利类型

  • 公开/公告日1975-02-03

    原文格式PDF

  • 申请/专利权人 SANDOZ AG;

    申请/专利号DK19700001730

  • 申请日1970-04-07

  • 分类号C07D221/16;

  • 国家 DK

  • 入库时间 2022-08-23 04:42:06

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