摘要:

AbstractThis review article comprises tetracyclic rigid analogues of phenothiazine and dibenzothiazepine derivatives. In order to discover new useful drugs, the side chain of the heterocyclic nucleus is incorporated into a ring forming tetracyclic compounds. The text has been divided in thirteen sections.

ISSN:0022-152X    

DOI:10.1002/jhet.5570290401

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

Abstract1′‐Halogenomethyl, 1′‐azidomethyl and 1′‐disubstituted aminomethyl derivatives of BAU (5‐benzylacyclouridine) and BBAU (5‐benzyloxybenzylacyclouridine) were synthesized in the course of our studies of benzylacyclouridines. Two new and more convenient preparations of the previously known aminomethyl‐and hydroxymethyl‐parent compounds of these two series, AM‐BAU, AM‐BBAU and HM‐BBAU are also reported. These compounds were synthesized during a search for potential antiviral agents and pyrimidine

ISSN:0022-152X    

DOI:10.1002/jhet.5570290402

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

AbstractA general synthesis for the preparation of a series ofN‐bridgehead compounds: pyrroloimidazopyridine, pyrimidine and naphthyridine has been developed beginning with azidovinyl compounds with thermolytic or photochemical metho

ISSN:0022-152X    

DOI:10.1002/jhet.5570290403

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

AbstractMetalation of pivalamidopyrazine andN‐t‐butylpyrazinamide were studied. For pivalamido pyrazine the yields were poor and some addition products were isolated. The metalation oft‐butylpyrazinamide was successful and a curious regioselectivity was highli

ISSN:0022-152X    

DOI:10.1002/jhet.5570290404

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

AbstractA one‐pot preparation of carboximidamides (amidines)11–14involves treatment of amides2–5with phosphorus pentachloride followed by the treatment of the resultant crude imidoyl chlorides7–10with ammonia. Amidines11–14are cyclized to quinazolines20–26in lithium alkylamide‐or dialkylamide‐med

ISSN:0022-152X    

DOI:10.1002/jhet.5570290405

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

AbstractThe synthesis of thesyn‐14andanti‐13isomers of 2(S)‐phthalimidornethyl‐2,3,4,4a,7,7a‐hexahydro‐6‐oxo‐5H‐pyrano[2,3‐b]pyrrole was accomplished starting from sodium 3,4‐dihydro‐2H‐pyran‐2‐carboxylate. The isomers were separated by preparative high performance liquid chromatography. Both isomers can serve as β‐bend mimetics and represent three amino acids plus the amino group of the fourth amino acid of a peptide. The lactam nitrogen was alkylated to provide the equivalent of a leucine

ISSN:0022-152X    

DOI:10.1002/jhet.5570290406

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

AbstractSeveral diazomethyl and diazoester substituted thiazoles and thiadiazoles were prepared and their ring/chain equilibria studied by nmr spectroscopy. The diazomethyl derivatives17a,b,dand19aexist predominantly or exclusively in the triazole form. Ring‐opening is promoted by introducing an ester group at the diazo function(17c,e, 19b, 21)or by changing thiazoles for thiadiazoles in the following order: thiazole<1,3,4‐thiadiazole<1,2,4‐thiadiazole. The diazoimine/triazole equilibria are also shifted towards the diazo form by raising the temperature and by using less polar solvents in the order: dimethyl sulfoxide

ISSN:0022-152X    

DOI:10.1002/jhet.5570290407

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

AbstractThree 1‐aryl‐2,5 pyrrolidinediones, two of which are novel, were prepared by reaction of the requisite primary aromatic amines with succinic anhydride, followed by treatment with acetic anhydride. The1H nmr spectra for the derivatives in which aryl is 1‐naphthyl and 1‐anthracenyl exhibit 32‐line multiplets for the four aliphatic hydrogens, indicating that all four are in different environments. Examination of molecular models demonstrates that the pyrrolidinedione and aryl ring systems cannot be coplanar and that rotation about the nitrogen‐aryl bond is restricted. Molecular mechanics calculations reveal that a dihedral angle of 50–65° for the two ring systems results in the minimum steric inte

ISSN:0022-152X    

DOI:10.1002/jhet.5570290408

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

AbstractA series of 3,7‐dimethyl‐9‐amino‐3,7‐diazabicyclo[3.3.1]nonane‐9‐carbonitrile and 3,7‐dimethyl‐9‐amino‐3,7‐diazabicyclo[3.3.1]nonane‐9‐carboxamideN‐substituted have been synthesized and studied by1Hand13C nmr spectroscopy and the crystal structure of 3,7‐dimethyl‐9‐benzylamino‐3,7‐diazabicyclo[3.3.1]nonane‐9‐carboxamide dihydrochloride (IVb·2HCl) has been determined by X‐ray diffraction. The compounds studied display in deuteriochloroform, dimethyl sulfoxide‐d6and methanol‐d4the same preferred flattened chair‐chair conformation with the methyl groups in equatorial position. The carboxamido group lies in a plane nearly perpendicular to the bispidine skeleton. The conformation and protonation sites ofIVb·2HCl in the crysta

ISSN:0022-152X    

DOI:10.1002/jhet.5570290409

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY

摘要:

AbstractThe reactions of 1‐(bromoalkyl)‐5‐bromo‐6‐bromomethyl‐3‐methyl‐2,4(1H,3H)‐pyrimidinedione(1)with several nucleophiles were examined as follows: by reaction with sodium methoxide, 6‐(bismethoxy)methyl‐5‐debrominated derivatives2, 3, and4were prepared; the corresponding di‐substituted compounds (side chains in 1‐and 6‐positions)5, 6, 7, and9were obtained by treatment with silver nitrate, silver acetate, potassium thiocyanate, and potassium thioacetate; the reaction with thioacetamide andiso‐butylamine gave bicyclic compounds [1,4]thiazino[4,3‐c]‐11, pyrazino[1,2‐c]‐12, and [1,4]diazepino[1,2‐c]pyrimidinedione13, respectively; pyrrolidine, morpholine, and sodium azide afforded the correspon

ISSN:0022-152X    

DOI:10.1002/jhet.5570290410

出版商:Wiley‐Blackwell    

年代:1992

数据来源: WILEY