| 摘要 |
<p>1504424 Isoquinoline derived aminoethers BEECHAM GROUP Ltd 5 Aug 1976 [9 Aug 1975] 33283/75 Heading C2C The invention comprises compounds of formula and salts thereof wherein R 1 is a C 1-6 alkyl, C 3-6 cycloalkyl phenyl, naphthyl, aralkyl, substituted phenyl or substituted naphthyl group; R 2 is a group: wherein R 6 is a hydrogen atom or a C 1-6 alkyl group, R 7 is a hydrogen atom or a C 1-6 alkyl, phenyl, tolyl, or benzyl group or R 6 is linked to R 7 so that the NR 6 R 7 moiety is a 5-, 6- or 7- membered ring, R 8 is a hydrogen atom or a C 1-4 alkyl group or is joined to R 6 to form part of a morpholino ring and R 9 and R 10 are each hydrogen atoms or C 1-4 alkyl groups; R 3 is a hydrogen atom or a C 1-6 alkyl or a trifluoromethyl group; R 4 is a hydrogen atom or a C 1-6 alkyl, benzyl or phenyl group or an acyl group containing from 2 to 7 carbon atoms and R 5 is a hydrogen atom or a C 1-6 alkyl group. In examples, these compounds are prepared by (1) reacting a 7-methoxy-2,3-dihydroisoquinolin - 4(1H) - one with R 1 -Li to give a 4 - R 1 - 7 - methoxy - 1,2,3,4 - tetrahydroisoquinolin - 4 - ol, treating the latter with ethanolic HCl followed by NaBH 4 to give the 4 - R 1 - 7 - methoxy - 1,2,3,4 - tetrahydroisoquinoline, optionally reacting with CH 2 O followed by H 2 /Raney Ni so as to introduce a 2- methyl group, treating with HBr to afford the 7-hydroxy analogue and etherifying with an R 2 - containing reagent; (2) reacting the 7- glycidyloxy analogue with R 6 R 7 NH; or (3) hydrogenolysing the R 7 = benzyl group to R 7 = H; or (4) separating optical isomers. Therapeutic compositions comprise the above tetrahydroisoquinolines, and may be administered orally or parenterally.</p> |
