摘要:

AbstractTwo mesitylene‐bridged hexaazamacrobicyclic ligands1and2were prepared by a three‐step process from available 2,4,6‐tris(bromomethyl)mesitylene (9) andN, N'‐di‐p‐tosylethylenediamine andN, N'‐di‐p‐tosyl‐1,3‐diaminopropane. First, mono‐BOC‐protected ditosylamines5and6were prepared by treating the two diamines with BOC‐O‐BOC. These mono‐BOC‐protected diamines were treated with the tris(bromomethyl)‐mesitylene followed by deprotection to give 2,4,6‐tris(2,5‐ditosyl‐2,5‐diazapentyl)mesitylene (3) and its 2,6‐diazahexyl analog4. These latter intermediates were treated with tris(bromomethyl)mesitylene to give the mesitylene‐bridged hexaazamacrobicycles. This three‐step

ISSN:0022-152X    

DOI:10.1002/jhet.5570330101

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractThe synthesis of a series of derivatives of 4‐hydroxycoumarin analogues of aflatoxin and a preliminary testing of their anticoagulant activity is describe

ISSN:0022-152X    

DOI:10.1002/jhet.5570330102

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractThe acid catalyzed reaction of 3‐thiophenamines with aldehydes in the presence of selenophenol as the reducing agent, gives 2‐alkyl‐3‐miophenamines. Without reduction, bis(3‐amino‐2‐thienyl)methane derivatives have been obtained and transformed into dithieno[3,2‐b:2′,3′‐e]pyridines by thermal and acidic treatment when the substrates are primary amines. These new tricyclic heterocycles can be synthesized in a one‐pot procedu

ISSN:0022-152X    

DOI:10.1002/jhet.5570330103

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractPhotocyclization reactions were carried out on 8‐alkoxy‐1,2,3,4‐tetrahydro‐1‐naphthalenones (six‐membered ring ketones)4a‐gand 4‐alkoxy‐6,7,8,9‐tetrahydro‐5H‐benzocyclohepten‐5‐ones (seven‐membered ring ketones)5a‐e in acetonitrile. Irradiation of4a‐fgave rearranged naphthyl alcohols8a‐fas major products. In the case of4g, 2a,3,4,5‐tetrahydronaphtho[1,8‐bc]furan‐2a‐ol6gwas obtained. In contrast, irradiation of5a‐eafforded 2,2a,3,4,5,6‐hexahydrocyclohepta[cd]benzofuran‐2a‐ols9a‐ein good yields. The difference in reactivities between4a‐gand5a‐eis attributed to the conformation of six‐ and seven‐membered rings. Conformational and substituent effects in cyclization step

ISSN:0022-152X    

DOI:10.1002/jhet.5570330104

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractThe first asymmetric synthesis of 3‐alkoxycarbonyl‐2‐amino‐4‐aryl‐4H‐naphtho[1,2‐b]pyrans, by Michael addition of 1‐naphthol to chirally modified arylidenecyanoacetates6and7, is described. Good yields and low diastereomeric excesses have been obtained in the 1,4‐conjugate additions. The absolute stereochemistry at C‐4 in major isomers of pyrans8and9has been assigned as 5 by X‐ray a

ISSN:0022-152X    

DOI:10.1002/jhet.5570330105

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractA series of analogues of 2‐phenylmorpholines with alkyl substituents at the C‐3 position were synthesized for anti‐tetrabenazine (anti‐TBZ) testing in mice. The target compounds were prepared by reaction of (2‐bromoalkyl) phenyl ketones21a‐hwith the appropriate aminoalcohol20a‐bto form morpholinols22a‐h. Hydride reduction of the morpholinols gave aminodiols23a‐hwhich were cyclized to morpholines6, 8, 10–12, 14–16, 18and19by acid catalaysis. Compounds7, 9, 13and17were prepared by reductive formylation. The smaller straight chain substituents of6, 8, 12and15, and thebetabranching of theiso‐butyl group of16were well tolerated; anti‐tetrabenazine ED50′swere comparable to compounds2–5. The α‐branched,N‐methylated, and side chain

ISSN:0022-152X    

DOI:10.1002/jhet.5570330106

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractCertain 1,2,4‐trisubstituted imidazoles underwent electrophilic attack of azodicarbonyl compounds on the 5‐position to form 5‐(1,2‐dialkoxycarbonyl)hydrazino‐ and 5‐(4‐phenyl‐3,5‐dioxo‐1,2,4‐triazolidin‐1‐yl)imidazole derivatives in moderate to high yields. The reaction was highly susceptible to the nature and the substitution pattern of the substituents on the imidazole ring. Thus 1,4‐di‐ or 1,2,5‐trisubstitued imidazoles, and 2‐methylsulfinylimidazoles gave no reaction. Reductive cleavage of the tetrasubstituted imidazoles with zinc dust‐acid gave the 1‐ or 1,2‐cleaved product depending upon the reaction temperature, b

ISSN:0022-152X    

DOI:10.1002/jhet.5570330107

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractNew substituted pyrido[2,3‐d]pyrimidines5and6have been prepared in one‐step from the readily available 6‐amino‐2,4‐dioxotetrahydropyrimidine (1) or 6‐amino‐4‐oxo‐2‐thioxotetrahydropyrimidine (2) and the arylidene substituted Meldrum's acid. The substitution pattern of the ethylene moiety in compounds5and6results in a strongpush‐pullelectronic effect. The semiempirical calculations using the AM1 method reveal two equally favoured conformations showing a distorted geometry. The calculated charge density values confirm the observed13

ISSN:0022-152X    

DOI:10.1002/jhet.5570330108

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractThe formation of a novel ring system, furo[2,3‐h][1,6]naphthyridineviathe Smiles rearrangement and intramolecular cyclization is described. Cyclization of 5‐(ω‐hydroxyalkylamino)‐8‐methyl‐1,2‐dihydrofuro[2,3‐h][1,6]naphthyridines provided novel spiro compound wi

ISSN:0022-152X    

DOI:10.1002/jhet.5570330109

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY

摘要:

AbstractThe title compounds5, 7and9which are the first arene sulfides of 7,8‐dihydrobenz[a]anthracene, 8,9‐and 10,11‐dihydrobenzo[a]pyrene, respectively, have been synthesized by treatment of the corresponding arene oxides4, 6and8withN,N‐dimethylthioformamide in the presence of catalytic amounts of trifluoroacet

ISSN:0022-152X    

DOI:10.1002/jhet.5570330110

出版商:Wiley‐Blackwell    

年代:1996

数据来源: WILEY