Verfahren zur Herstellung von 1-Aminoalkyl-1-arylindenen

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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description 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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(claimed) of general formula (I) where Ar = C6H5 (opt. substd. by halogen, alkyl, dialkyl, alkoxy, dialkoxy) (alkyl and alkoxy is not &gt; 4C) R1 = H, C6H5, alkyl (is not &gt; ca. 6C) Alk =alkylene (2-6C; 2-3C separating N from ring) R2,R3=alkyl (1-6C) or NR2R3 = N-substd. heterocyclic (is not &gt; 6C) R4 = H, Cl, Br, alkyl, alkoxy, dialkoxy (all is not &gt; 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). 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MAJEWSKI,ROBERT</creatorcontrib><creatorcontrib>M. BERDAHL,JAMES</creatorcontrib><title>Verfahren zur Herstellung von 1-Aminoalkyl-1-arylindenen</title><description>1. Cpds. (claimed) of general formula (I) where Ar = C6H5 (opt. substd. by halogen, alkyl, dialkyl, alkoxy, dialkoxy) (alkyl and alkoxy is not &gt; 4C) R1 = H, C6H5, alkyl (is not &gt; ca. 6C) Alk =alkylene (2-6C; 2-3C separating N from ring) R2,R3=alkyl (1-6C) or NR2R3 = N-substd. heterocyclic (is not &gt; 6C) R4 = H, Cl, Br, alkyl, alkoxy, dialkoxy (all is not &gt; 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.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1972</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZLAISy1KS8woSs1TqCotUvBILSouSc3JKc1LVyjLz1Mw1HXMzczLT8zJrszRNdRNLKrMycxLSc1LzeNhYE1LzClO5YXS3AwKbq4hzh66qQX58anFBYnJQFUl8S6uhmaGFuYGJo6GxkQoAQCYIS2a</recordid><startdate>19720413</startdate><enddate>19720413</enddate><creator>F. MAJEWSKI,ROBERT</creator><creator>M. BERDAHL,JAMES</creator><scope>EVB</scope></search><sort><creationdate>19720413</creationdate><title>Verfahren zur Herstellung von 1-Aminoalkyl-1-arylindenen</title><author>F. MAJEWSKI,ROBERT ; M. BERDAHL,JAMES</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_DE1618704A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>ger</language><creationdate>1972</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>F. MAJEWSKI,ROBERT</creatorcontrib><creatorcontrib>M. BERDAHL,JAMES</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>F. MAJEWSKI,ROBERT</au><au>M. BERDAHL,JAMES</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Verfahren zur Herstellung von 1-Aminoalkyl-1-arylindenen</title><date>1972-04-13</date><risdate>1972</risdate><abstract>1. Cpds. (claimed) of general formula (I) where Ar = C6H5 (opt. substd. by halogen, alkyl, dialkyl, alkoxy, dialkoxy) (alkyl and alkoxy is not &gt; 4C) R1 = H, C6H5, alkyl (is not &gt; ca. 6C) Alk =alkylene (2-6C; 2-3C separating N from ring) R2,R3=alkyl (1-6C) or NR2R3 = N-substd. heterocyclic (is not &gt; 6C) R4 = H, Cl, Br, alkyl, alkoxy, dialkoxy (all is not &gt; 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.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title Verfahren zur Herstellung von 1-Aminoalkyl-1-arylindenen
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