首页> 外国专利> METHOD OF NEW (4ARS,5SR,9BSR)-AND (4ARS,5SR,9BRS)1,3,4,4A,5,9B-HEXAHYDRO-5-PHENYL-2H-INDENO-(1,2,-D)PYRIDINES MAKING

METHOD OF NEW (4ARS,5SR,9BSR)-AND (4ARS,5SR,9BRS)1,3,4,4A,5,9B-HEXAHYDRO-5-PHENYL-2H-INDENO-(1,2,-D)PYRIDINES MAKING

机译:新的(4ARS,5SR,9BSR)-和(4ARS,5SR,9BRS)1,3,4,4A,5,9B-六氢-5-苯基-2H-茚基-(1,2,-D)吡啶的方法制造

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。

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