摘要:

AbstractAlkylation of the sodium salt and the trimethyl silylated derivatives of 6‐methyl‐1,2,4‐triazin‐3(4H)‐one 1‐oxide with chloromethoxyethyl acetate, n‐hexyl chloride and benzyl bromide gave the 4‐substituted products. However, attempts to achieve the ring closure ofN4‐(2‐acetoxyethoxymethyl)thiosemicarbazide with bicarbonyl compounds to the correspondingas‐triazines under different reaction conditions was not possible without disruption of the acetoxyethoxymethyl moiety. Although theas‐triazine nucleoside analog II did not show antileukemic activity, this and other 4‐alkylatedas‐triazine 1‐oxides revealed good growth inhibitory effects against a representati

ISSN:0022-152X    

DOI:10.1002/jhet.5570230601

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

AbstractSelective photodeuteration of carboxyltryptamines at C‐4 allowed to settle the controversy about the13C nmr assignment of C‐4, C‐5 and C‐6, which for tryptophan are definitively assigned at 118.4, 118.2 and 120.6 ppm, respe

ISSN:0022-152X    

DOI:10.1002/jhet.5570230602

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

AbstractFrom the condensation of 5‐hydroxymethyluracil and glycerine, 5‐[(2,3‐dihydroxy‐1‐propoxy)methyl]uracil (3) was synthesized, which was converted to the isocytosine derivative9by the ring‐transformation reactionviadimethyluracil

ISSN:0022-152X    

DOI:10.1002/jhet.5570230603

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

AbstractReaction of 1‐naphthol with 2‐chlorocyclohexanone in alkaline alcohol gave as the major product 5‐(2′‐oxocyclohexyl)‐7,8,9,10‐tetrahydronaphtho[1,2‐b]benzofuran (1), which could be converted to the title compound 5 by reduction and dehydrogenation. This product arises from ambident alkylation of 1‐naphthol at the 2‐and 4‐positions.Viathe 2′‐oxocyclohexyl ether, 5 was also synthesized

ISSN:0022-152X    

DOI:10.1002/jhet.5570230604

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

AbstractThe reaction of 2‐mercaptobenzothiazole, 2‐mercaptobenzoxazole or 5‐chloro‐2‐mercaptobenzothiazole with either acrylonitrile or acrylamide under basic conditions afforded theN‐cyanoethylated products1, 2and3or theN‐amidoethylated products4, 5and6, respectively. The reaction of the sodium salts of the same thiazolethiols with 3‐chloropropionitrile furnished a mixture containing theN‐cyanoethylated products1, 2and3and the unknownS‐cyanoethylated products 7,8and9, respectively. Whereas, substituting 3‐chloropropionamide for 3‐ chloropropionitrile in the same reaction gave only theS‐substituted products10, 11, and12, respectively. The treatment of10, 11or12with phosphorus oxychloride or thionyl chloride in DMF afforded7, 8and9in excellent yields. Possible mechanisms and supporti

ISSN:0022-152X    

DOI:10.1002/jhet.5570230605

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

Abstract4‐Methylfuro[3′,2′:5,6]benzofuro[3,2‐c]pyridine (3) was synthetized from 2‐acetylfuro[3,2‐f]benzo[b]furan (4) or from 2‐acetyl‐5,6‐dihydrofuro[3,2‐f]benzo[b]furan (10). The key step involves a rearrangement‐cyclization of azides6and12to form 4‐methylfuro[3′,2′:5,6]benzofuro[3,2‐c]pyridin‐1(2H) one (7) and 8,9‐dihydro‐4‐methylfuro[3′,2′:5,6]benzofuro[3,2c]pyridin‐1(2H)‐one (13). Introduction of an aminoalkyl chain on carbon 1 was effected by substitution of 1‐chloro‐4

ISSN:0022-152X    

DOI:10.1002/jhet.5570230606

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

AbstractDie kathodische Reduktion von Pyridin‐2,3‐dicarbonsäure‐N‐phenylimid (1) unter aprotischen Bedingungen in Gegenwart von Trimethylchlorsilan führt zu 2‐Phenyl‐1,3‐bis[trimethylsilyloxy]‐pyrrolo‐[3,4‐b]pyridin (4), das mit elektronenarmen Olefinen über eine Cycloaddition in Chinolinderivate überführt werden kann.Aus Pyrazin‐2,3‐dicarbonsäure‐N‐phenylimid (3) entsteht unter gleichen Bedingungen 2‐Phenyl‐1,3‐bis‐[trimethylsilyloxy]‐pyrrolo[3,4‐b]pyrazin (13), das nicht mehr ausreichend stabil ist. Darstellung von13in Gegenwart eines Dienophils führt jedoch zu Chinoxalinderivaten als Abfangprodukte.Die orthochinoiden Heterocycle

ISSN:0022-152X    

DOI:10.1002/jhet.5570230607

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

AbstractSynthesis of new 2,1‐benzisothiazoline 2,2‐dioxides1and some of its benzene ring substitution derivatives was accomplished by two different methods of cyclisation. Also a number of newN‐substituted derivatives, obtained by treatment of1and analogues with aliphatic and aromatic acid chlorides are desc

ISSN:0022-152X    

DOI:10.1002/jhet.5570230608

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

AbstractA number of variations and derivatives of BAU (5‐benzylacyclouridine) and BBAU (5‐benzyloxybenzylacy‐clouridine), potent inhibitors of uridine phosphorylase were synthesized for evaluation as potential cancer chemotherapeutic agents. (“Acyclo” = 2′‐hydroxymethoxymethyl‐). These included a modification of the methylene group at N‐1, esters of the terminal hydroxyl of the acyclo group, and extension of the benzyl chain at position 5 of the uracil base. BBBAU was a very good potentiator of FUd

ISSN:0022-152X    

DOI:10.1002/jhet.5570230609

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY

摘要:

AbstractReaction of benzamide oxime (1) withN, N′‐dicyclohexylcarbodiimide (2) afforded 5‐cyclohexylamino‐3‐phenyl‐1,2,4‐oxadiazole (3),N, N′,N″‐tricyclohexylguanidine (4) andN, N′‐dicyclohexyl urea (5). When acetone (8a) or ethyl acetoacetate (8b) was added as a trap, the yield of3increased slightly andN‐(2‐propylidene)cyclohexylamine (9a) or ethyl 3‐cyclohexylamino‐2‐butenoate (9b) was obtained as well as products4and5. Acetylacetone (8c) and diacetyl (8d) were also used as the trap for the cyclohexylamino group. Whenp‐toluenesulfonic acid was added as a catalyst, 1‐cyclohexyl‐5‐cyclohexylamino‐3‐phenyl‐1

ISSN:0022-152X    

DOI:10.1002/jhet.5570230610

出版商:Wiley‐Blackwell    

年代:1986

数据来源: WILEY