摘要:

AbstractWith the help of drug design, 8‐, 9‐, 10‐ and 11‐methylacronycines24, 25, 26and27have been selected and synthesised to improve the cytostatic potency of acronycine (31). The condensation of phloroglucinol with 6‐methylanthranilic acid gave 7‐hydroxy‐1,9‐dimethyldibenzo[b,j][1,7]phenanthroline‐8,14(5H,13H)‐dione (32)

ISSN:0022-152X    

DOI:10.1002/jhet.5570300601

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractThe cyclocondensations of benzofuroxan1awith carbonyl compounds were smoothly and efficiently carried out by the adsorption of the components on the surface of silica gel or a molecular sieve to form a 2,3‐disubstituted quinoxaline 1,4‐dioxide. When the reactions using a molecular sieve 3A (powder) were carried out at 90°, the actual reaction times were reduced to 0.5‐2 hours. Although Duerckheimer has reported the isolation of only the 7‐substituted quinoxaline 1,4‐dioxide when 5‐methoxybenzofuroxan1ewas allowed to react with ethyl acetoacetate2j, it produced only the 6‐methoxy isomer as the reaction product by our method. 5‐Carboxybenzofuroxan1fdid not react with the c

ISSN:0022-152X    

DOI:10.1002/jhet.5570300602

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractThe synthesis of the title compounds 5H,12H‐[1]benzoxepino[4,3‐b]indol‐6‐ones10was effected by the Fischer indole cyclization of some 2,3‐dihydro‐4‐phenylhydrazono[1]benzoxepin‐5‐ones9, obtained from the 3,4‐dihydro‐4‐hydroxymethylene[1]benzoxepin‐5(2H)‐ones7by the Japp‐Klingemann reaction. The structure of these new heterocyclic compounds was supported by i

ISSN:0022-152X    

DOI:10.1002/jhet.5570300603

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractThe new 22‐π, aromatic “pentaplanar” macrocycle, ozaphyrin (6), has been synthesized by a McMurry coupling of 5,5′‐diformyl‐4,4′‐dipropyl‐2,2′‐bipyrrole (1) with 2,5‐bis(5‐formyl‐4‐propyl‐2‐pyrrolyl)furan (5). This synthetic pathway to ozaphyrin and its characterization by1H nmr spectroscopy, uv‐visible spectroscopy, cyclic voltammetry, and X‐ray crystallography are described. The structure consists of layers of planar, staggered macrocycles stacked perpendicular to the α‐axis. Ozaphyrin crystallizes with four formula units in the monoclinic space group C52h‐P21/nin a cell of dimensions a = 10.481(7) Å, b = 17.353(17) Å, c = 18.726(12) Å, and β = 102.84(5)° (108 K). The structure has been refined on F2(5171 unique reflections, 411 variables) to Rw(Fo2) = 0.165. The conventional agreement index R(F) is

ISSN:0022-152X    

DOI:10.1002/jhet.5570300604

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractThe lithiation of 2‐chloro, 2‐methoxy and 2‐pivaloylaminoquinoxaline was studied. In the case of 2‐chloro and 2‐methoxyquinoxaline the simultaneous formation of dimers could not be avoided. The resulting lithio derivatives were reacted with carbonyl compounds and iodine. Yields in excess of 50% were

ISSN:0022-152X    

DOI:10.1002/jhet.5570300605

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractA reaction of 2‐(2‐nitrobenzoylmethyl)‐1,3‐dioxolane (3) with hydroxylamine, followed by acid catalyzed cyclization, produced 5‐(2‐nitrophenyl)isoxazole (5) as the only isolable product, whereas 2‐(benzoylmethyl)‐1,3‐dioxolane (9) under identical conditions produced a 2.5:1 mixture of 3‐phenyl and 5‐phenylisoxazoles10and11. These findings contradict the literature report that β‐keto ethyleneacetals on treatment with hydroxylamine produce exclusively 3‐substituted isoxazoles. As an additional proof, 3‐(2‐nitrophenyl)isoxazole (8) was prepared by an unambiguous methodviathe nitrile oxide route for comparison. The intermediate obtained on treatment of 2‐(2‐nitrobenzoylmethyl)‐1,3‐dioxolane (3) with hydroxylamine was found to be an isomeric mixture of 5‐hydroxy‐5‐(2‐nitrophenyl)‐2‐isoxazoline (4) and thesynandantimono‐oximes19(at least in solution), either of which could give 5‐(2‐nitrophenyl)isoxazole (5) on acid treatment. A mechanisti

ISSN:0022-152X    

DOI:10.1002/jhet.5570300606

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractThe reaction of 2‐(alkylamino)‐3‐(trifluoroacetyl)butenedioates2a‐bwith alkyl and aryl hydrazines in ether provides 1,6‐dihydro‐6‐oxo‐3‐(trifluoromethyl)‐4‐pyridazinecarboxylates as their alkylamine salts3a‐g. The structures of these products are substantiated using 2D nm

ISSN:0022-152X    

DOI:10.1002/jhet.5570300607

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractStarting from [4,3‐c] and [3,2‐c] methyl chlorosulfonylthiophenecarboxylates the synthesis of ketones7and8is described. These compounds are the first two representatives of the new thieno[3,4‐c] and thieno‐[3,2‐c][2,1]benzothiazepine ring systems. The formation of methyl 3‐chlorosulfonylthiophene‐2‐carboxy‐lat

ISSN:0022-152X    

DOI:10.1002/jhet.5570300608

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

Abstract3‐Substituted 2(1H)‐pyridones are produced from reaction of 4‐(4‐morpholino)‐3‐pentenone1with each of the following carbon acids: cyanoacetamide, malononitrile, cyanothioacetamide, acetylacetamide, benzoyl‐acetonitrile. Reaction of ethyl 3‐(4‐morpholino)‐2‐butenoate2with cyanoacetamide gives the corresponding hydroxypyridone. Pyrimidines are formed by reaction of1and of2with benzamidine and with S‐benzylthio‐urea; in the last case, the eliminated morpholine displaces the benzylthio group

ISSN:0022-152X    

DOI:10.1002/jhet.5570300609

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractTetrazolyl‐substituted enamino ketones1react with various amidines2to give 5‐(1‐phenyl‐1H‐tetrazol‐5‐yl)pyrimidines3. In the case of the chloroacetyl enamine44‐(N,N‐dimethylaminomethyl)‐substituted tetra‐zolylpyrimidines5were obtained. Subsequent hydrolysis of the 4‐trifluoromethyl derivatives3b, 3dand3gafforded the corresponding 5‐(1‐phenyl‐1H‐tetrazol‐5

ISSN:0022-152X    

DOI:10.1002/jhet.5570300610

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY