摘要:

Abstract5‐Hexyl‐7‐(S‐methylsulfonimidoyl)xanthone‐2‐carboxylic acid1a, when heated above its melting point gives a number of products including the corresponding methyl ester1b, which arises by a novel methyl group transfer. A similar methyl transfer reaction is observed when the sulfoximide and carboxylic acid groups are present in differen

ISSN:0022-152X    

DOI:10.1002/jhet.5570160601

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

AbstractA synthesis of 5‐azaindole derivatives is described. This synthetic approach involves the preparation of an appropriately substituted pyrrole derivative by a 1,3‐dipolar cycloaddition reaction of dimethyl acetylenedicarboxylate with a mesoionic oxazolium 5‐oxide. The pyrrole intermediate contains a protected β‐aminoethyl substituent, and subsequent removal of the phthalimido protecting group results in cyclization to yield the corresponding 5‐azaindole. This approach has been used for both acyclic and cyclic amino acid precursors of the 1,3‐dipole which is ultimately used in

ISSN:0022-152X    

DOI:10.1002/jhet.5570160602

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

AbstractStableN‐(5‐aryl‐1,3,4‐oxadiazol‐2‐yl)phosphorimidic trichlorides (II) are obtained by refluxing 2‐amino‐5‐aryl‐1,3,4‐oxadiazoles (I) with one equivalent of phosphorus pentachloride in dry benzene. The reactions of the phosphorimidic trichlori

ISSN:0022-152X    

DOI:10.1002/jhet.5570160603

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

AbstractAmination of 5‐chloro‐6‐nitro‐2,4‐quinazolinediamine (2) afforded 6‐nitro‐2,4,5‐quinazolinetriamine (3) which was hydrogenated catalytically to produce 2,4,5,6‐quinazolinetetraamine (5). Condensation of5with the requisite diketones afforded 8,9,10,11‐tetrahydropyrimido[5,4‐a]‐phenazine‐1,3‐diamine (6), several pyrazino[2,3‐f]quinazoline‐8,10‐diamines (7–10,13) as well as two pyrimido[4,5‐f]phenazinediamines (11,12). Amination of2in the presence of formamide at 120° led to the formation of 9‐nitro‐1H‐pyrimido[4,5,6‐de]quinazolin‐5‐amine (4). None of these compounds showed suppressive activity when tested parenterally against lethalPlasmodium bergheiinfections in mice. When tested against various bacteriain vitro,7and10exhibited activity againstStrepto

ISSN:0022-152X    

DOI:10.1002/jhet.5570160604

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

Abstract3,4‐Dibenzoyl‐2‐oxobutyrate 4‐semicarbazone (6a), ethyl 2,4‐dioxo‐3‐phenacylvalerate 3‐semicarbazone (6b) and diethyl phenacyloxalectate 3‐semicarbazone (6c)viaacid catalysed intramolecular cyclization afforded 2‐phenyl‐4‐R‐3H‐imidazo[1,5‐d]pyridazine‐5,7‐(6H)diones (8d,e,f). Elemental analyses and spectroscopic data (ir, nmr, ms) were in good agree

ISSN:0022-152X    

DOI:10.1002/jhet.5570160605

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

AbstractBenzoylacetonitrile (II) reacted with trichloroacetonitrile (III) to yield the β‐amino‐β‐trichloromethylacrylonitrile IV. Compound IV reacted with hydrazine hydrate to yield 5‐amino‐4‐cyano‐3‐phenylpyrazole (V) and with 2‐aminopyridine to yield the aminopyridine derivative VIII (cf., Chart I). Compound IV reacted with III to yield 2,4‐bis(trichloromethyl)‐5‐cyano‐6‐phenylpyrimidine (I) which could be converted into a variety of pyrazolo[4,3‐d]pyrimidine derivatives by treatment with hydrazine hydrate under a variety of different experime

ISSN:0022-152X    

DOI:10.1002/jhet.5570160606

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

Abstract4‐Amino‐3‐cyanopyrazole (6) had once been considered to be a possible intermediate in the photochemical conversion at 350 nm of diaminomaleonitrile (1) into 4‐amino‐5‐cyanoimidazole (3), a precursor of adenine. The pyrazole was synthesized and irradiated at 350 nm. No isomerization into the imidazole was observed, even when the photolysis was carried out in the presence of an excess of1, where sensitization by this or one of its photolysis products might have operated. At 254 nm, complete decomposition of6was observed, with formation of polymeric products. At 300 nm,6underwent isomerization to3, as well as extensive decomposition. Hydrogen cyanide was probably produced, which reacted with the remaining starting material to yield 7‐aminopyrazolo[4,3‐d]pyrimidine (10), which did not isomerize into adenine under the photolysis conditions. A polymer was also obtained, from which glycine was identified a

ISSN:0022-152X    

DOI:10.1002/jhet.5570160607

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

AbstractThe title compounds were prepared by reaction of 3‐(2H)furanones and 2,3‐dihydro‐4‐pyrones with methylhydrazine or alternatively by methylation of the correspondingN‐unsubstituted pyrazoles.13C and1H nmr were used to assign the isomeric 3‐methyl or 5‐meth

ISSN:0022-152X    

DOI:10.1002/jhet.5570160608

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

AbstractThe cyclization of 2‐(2‐chloro(bromo)phenoxy)anilines and 3‐(phenoxy)pyridines to 10‐methylphenoxazines and 10‐methyl[1,4]benzoxazino[3,2‐b]pyridines, respectively, by means of dimethyl methylphosphonate is reported. The cyclization reaction proceeded with expulsion of methyl ether. Demethylation of some 10‐methylphenoxazines was achieved with pyridine hydrobromide. Nitration was carried out with sodium nitrite, and by reduction of the nitro groups the corresponding amines

ISSN:0022-152X    

DOI:10.1002/jhet.5570160609

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY

摘要:

AbstractCertain oximes were prepared from 2‐quinolylmethyl 2‐pyridinyl ketone and 2‐(1,10‐phenanthrolyl)methyl 2‐pyridinyl ketone. Also, the preparation of two series of hydrazones was effected: one from 2‐acetylquinoline and one from 2‐acetyl‐1,10‐phenanthroline. The latter compound and 2‐(2‐quinolyl)‐1,10‐phenanthroline were also synthesized. All the compounds were tested for their m

ISSN:0022-152X    

DOI:10.1002/jhet.5570160610

出版商:Wiley‐Blackwell    

年代:1979

数据来源: WILEY