ISSN:0022-152X    

DOI:10.1002/jhet.5570190101

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractA practical synthesis (Scheme I) is described for the preparation of a series of 4‐substituted‐3,3‐dimethyl‐1,2,3,4‐tetrahydroisoquinolines (3). Treatment of α‐(1‐amino‐1‐methylethyl)arylmethanols or α‐(1‐amino‐1‐methylethyl)heteroarylmethanols (5) with aromatic aldehydes gave imines7from which amino alcohols8were derived by reduction with potassium borohydride. Acid catalyzed cyclization of8yielded3. An acyl substituent was installed by Friedel‐Crafts acylation as a final step. The biological activities

ISSN:0022-152X    

DOI:10.1002/jhet.5570190102

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractFifteen new 3‐arylaminomethyl‐5‐(2‐hydroxy‐3,5‐dibromophenyl)‐1,3,4‐oxadiazole‐2‐thiones were synthesized and characterized by their sharp melting points, elemental analyses and ir spectra. These substituted oxadiazolylthiones were evaluated for their enzyme inhibitory activity. All compounds inhibitedin vitromonoamine oxidase and succinate dehydrogenase activity of rat brain homogenates. The degree of monoamine oxidase inhibition ranged from 59‐93% at a final concentration of 1 × 10−4Mwhereas the inhibition of succinate dehydrogenase was 49‐100% at a final

ISSN:0022-152X    

DOI:10.1002/jhet.5570190103

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractHydroxyl‐protected derivatives of 1‐ and 3‐(2‐hydroxyethoxymethyl)imidazoles (4,5,7‐10) have been prepared from 5‐amino‐4‐carbamoylimidazoles (2). The protected derivatives were converted to acyclic analogues of imidazole nucleosides (6) or subjected to various cyclisation reactions leading to 9‐(2‐hydroxy‐ethoxymethyl)‐substituted 2‐methyl‐, 2‐phenyl‐ and 2‐azahypoxanthines (18,13and20, respectively) and 1‐methylguanine (28). For assignment of structures to isomeric imidazole and purine derivatives

ISSN:0022-152X    

DOI:10.1002/jhet.5570190104

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractThe action of hydrazine hydrate on 5‐arylidene‐3‐aryl‐2‐methylmercaptohydantoins led to ring opening and rearrangement into 5‐arylidene‐3‐amino‐N2‐aryl‐glycocyamidines (9a‐f). The structure of the products9a‐fwas established and the mechanism of thei

ISSN:0022-152X    

DOI:10.1002/jhet.5570190105

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractTreatment of the diastereoisomericN‐(1‐phenylethyl)‐1,2‐diphenyl‐2‐aminoethanols with benzaldehyde yields stereospecificallyN‐(1‐phenylethyl)‐2,4,5‐triphenyloxazolidines with four chiral centers. The configurations of these oxazolidines are established through their ring‐opening reactions with methylmagnesium iodide and subsequent oxidation

ISSN:0022-152X    

DOI:10.1002/jhet.5570190106

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractIn reactions of 1‐phenyl‐1,4‐dihydro‐3‐(2H)benzoisoquinolinones with benzaldehyde in the presence of a strong base, the final result can be ring substitution with aromatization or only aromatization of the starting isoquinolinone, depending on the position of the ring junction ([f] or [h]), in the 5‐methyl derivative the latter process becomes predominating. In the system sodium hydride‐dimethylformamide, containing no aromatic aldehyde, methylation at site 4 occurs. Using compounds labelled with deuterium, it has been established that the 4‐benzyl or 4‐methyl derivatives with aromatic structures are formed through hydri

ISSN:0022-152X    

DOI:10.1002/jhet.5570190107

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractThe mass spectral fragmentation patterns of 5‐methyl‐4‐[(phenylamino)methylene]‐2,4‐dihydro‐3H‐pyrazol‐3‐one and its 2‐methyl and 2‐phenyl derivatives have been elucidated. The principal initial fragmentation route involves rupture of the exocyclic CH‐NH bond. Minor routes involve loss of H, OH and C6H5from the molecular ion and rupture

ISSN:0022-152X    

DOI:10.1002/jhet.5570190108

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractTreatment of 3‐aminobenzo‐as‐triazines with bromoacetaldehyde ethylene acetal give linear tricyclic imidazobenzo‐as‐triazines, where 3‐amino‐7‐methylbenzo‐as‐triazine 1‐oxide yields the angular isomer. The structures of these compounds have been established by comparing their nmr spectra to those of pyrazolo [5,1‐c]‐ ands‐triazolo[5,1‐c]benzo‐as‐triazines obtained form the appropriate azo derivati

ISSN:0022-152X    

DOI:10.1002/jhet.5570190109

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY

摘要:

AbstractReaction of diazoindenothiophenes (1and2) with benzoyl acetylene (4) afforded the rearrangement products (6aandb) of the initial adducts. The major product of the reaction of diazo indenothiophene (3) with4was butadiene derivative8a. Reaction of1with dibenzoylacetylene (5a) gave the rearranged pyrazole (12), while the reaction of2and3, afforded the butadiene derivatives (8b‐d

ISSN:0022-152X    

DOI:10.1002/jhet.5570190110

出版商:Wiley‐Blackwell    

年代:1982

数据来源: WILEY