Verfahren zur Herstellung von 3-Aminoalkyl-3-arylindanolen-1
1. Cpds. (claimed) of general formula (I) where Ar = C6H5 (opt. substd. by halogen, alkyl, dialkyl, alkoxy, dialkoxy) (alkyl and alkoxy is not > 4C) R1 = H, C6H5, alkyl (is not > ca. 6C) Alk =alkylene (2-6C; 2-3C separating N from ring) R2,R3=alkyl (1-6C) or NR2R3 = N-substd. heterocyclic (is...
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Zusammenfassung: | 1. Cpds. (claimed) of general formula (I) where Ar = C6H5 (opt. substd. by halogen, alkyl, dialkyl, alkoxy, dialkoxy) (alkyl and alkoxy is not > 4C) R1 = H, C6H5, alkyl (is not > ca. 6C) Alk =alkylene (2-6C; 2-3C separating N from ring) R2,R3=alkyl (1-6C) or NR2R3 = N-substd. heterocyclic (is not > 6C) R4 = H, Cl, Br, alkyl, alkoxy, dialkoxy (all is not > 4C) 2. Acid addition salts of (I) 3. Na and K salts of (I). Includes diastereoisomers of (I). Simple unambiguous synth. affords pure (IV) in very high yield free from undesired by-products. In addition, (I) have various pharmacological activities per se; thus (I; R4 = H, NR2R3=NMe2, Ar=C6H5, Alk=CH2CH2, R1=H (cpd.A) and Me) are active in preventing the phenylquinone writhing syndrome in mice (cf. analgesics), and effective in preventing reserpine-induced ptosis in mice (cf. antidepressants). (A) at 10 mg./kg. in anaesthetized dogs causes marked hypotensive and intestinal relaxant effects. |
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