摘要:

AbstractThe Beckmann rearrangement of steroidal oximes is reported. Different methods of esterification of homo‐aza‐steroids with carboxylic derivatives ofN,N‐bis(2‐chloroethyl)aniline are reported.The lipophilic nature of the steroidal hormones is the reason for searching compounds containing as the biological platform the steroid molecule and as the active moiety the alkylating agent, such as nitrogen mustards linked to the steroid with a stable bond or with an easily cleaved ester or ether molecule and different other active species, hopefully to transport and deliver the alkylating agent to the specific target tissue. The concept to design hybrid compounds containing as the biological platform steroidal lactams and as the alkylating congener carboxylic derivatives ofN,N‐bis(2‐chloroethyl)aniline might form compounds with synergistic activity.The findings suggest that the conformation of the alkylating agent influences the anticancer activity, while the amide group of the lactam molecule is important for activity in L1210 leukemia.These hybrid compounds with a modified steroid as the biological platform furnish derivatives with advantages compared to the unmodified steroids with alkylating agents.Different methods of esterification of homo‐aza‐steroids with carboxylic derivatives ofN,N‐bis(2‐chloro‐ethyl

ISSN:0022-152X    

DOI:10.1002/jhet.5570300101

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractSome [1,2,4]triazolo[1,5‐c]quinazolin‐5(6H)‐ones7, the corresponding isomers [1,2,4]triazolo[4,3‐c]quinazo‐lin‐5(6H)‐ones and the 5‐amino derivatives8, 9and11have been synthesized starting from the acylamidrazones5. The preparation of 5H‐[1,2,4]triazolo[1,5‐d]‐1,4‐benzodiazepin‐6(7H)‐ones15and of 5‐cyclicaminomethyl‐[1,2,4]triazolo[1,5‐c]qu

ISSN:0022-152X    

DOI:10.1002/jhet.5570300102

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractA series of substituted quinaldines was synthesized with much improved yields from the reaction of croton‐aldehyde and the corresponding anilines using eitherp‐chloranil or 2,3‐dichloro‐1,4‐naphthoquinone as th

ISSN:0022-152X    

DOI:10.1002/jhet.5570300103

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractA synthesis of the 4,5‐dihydro derivatives of the previously known pyrazolo[3,4‐a]acridine ring system is described. The reaction of a 3,4‐dihydroacridin‐1(2H)‐one withN,N‐dimethylformamide dimethyl acetal gave a reactive enamino ketone, which yielded the desired heterocycle upon reaction with hydrazine. Using this chemistry, 11‐amino‐4,5‐dihydro‐2H‐pyrazolo[3,4‐a)acridine (3) and a number of its 2‐substituted derivatives4a‐kwere synthesized and evaluated as acetylcholinesterase inhibitors, based on their relationship to 1,2,3,4‐tetrahydro‐9‐acridinamine (THA). 1‐Amino‐4,5‐dihydro‐1H‐pyrazolo[3,4‐a]acridine (11a) and 2‐amino‐4,5‐dihydro‐1H‐pyrazolo[3,4‐a]acridine (11b) were also synthesize

ISSN:0022-152X    

DOI:10.1002/jhet.5570300104

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractThe infrared spectra in several media and the crystal structure of 3‐methyl‐2,4‐diphenyl‐3‐azabicyclo[3.3.1]‐nonan‐9β‐ol (I) (Scheme I) have been determined, in order to complete the structural study described for the title compound from the1H and13C nmr data [1]. The bicyclic system adopts a flattened chair‐chair conformation in which the cyclohexane ring is more flattened. The methyl and phenyl groups are in equatorial positions and the OH group in an axial position with respect to t

ISSN:0022-152X    

DOI:10.1002/jhet.5570300105

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractThe reaction between 2‐substituted ethyl 2,5‐dihydro‐5‐oxoisoxazole‐4‐carboxylates (2a,b) and heterocyclic amines1, 4, and6, having the amino group in position 2 with respect to the nuclear nitrogen afforded fused pyrimidine

ISSN:0022-152X    

DOI:10.1002/jhet.5570300106

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractTrifluoro or pentafluoroacylation of heteroaryl‐enamines2a,bgave the corresponding perfluoroacylated heteroaryl‐enamines3a‐c. Heating the latter compounds with diethyl iminomalonate gave 2‐amino‐3‐pyridinecarboxylates4a‐c. Hydrolysis to the free acids5a‐c, and reaction with diphenylphosphoryl azide afforded the desired 1,3‐dihydro‐6‐heteroaryl‐5‐perfluoroalkyl‐2H‐imi

ISSN:0022-152X    

DOI:10.1002/jhet.5570300107

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

Abstract7‐Arylidene‐2H,6H‐naphtho[1,8‐bc]furan‐2,6‐diones3were prepared by a retro‐Diels‐Alder reaction of the corresponding dihydro 1,3‐oxazines2or in a one pot synthesis from 6‐hydroxy‐2H‐naphtho[1,8‐bc]furan‐2‐one1. TheirEconfiguration was established from the chemical shift's values of the vinylic proton and by1H nmr NOE difference spectroscopy. Cycloadditions of3bupon styrene or stilbene were catalyzed by boron trifluoride etherate. The cycloadducts were obtained with t

ISSN:0022-152X    

DOI:10.1002/jhet.5570300108

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractSynthesis of pyridazino[1,2‐a][1,2,4]benzotriazin‐6‐one derivatives involving reaction of either 1,2,3,6‐tetra‐hydropyridazine (9) or hexahydropyridazine14with 2‐fluoro‐5‐nitrophenylisocyanate (5) to give,viaintramolecular cyclization,3aand16respectively is described. Compound3awas converted to18viamethylation and hydroxylation to give20followed by conversion to the acetonide derivative18. Both16and18were reduced to the amino derivatives17an

ISSN:0022-152X    

DOI:10.1002/jhet.5570300109

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY

摘要:

AbstractAddition of methylhydrazine to a variety of haloalkyl‐substituted α,β‐unsaturated esters gives 1,5‐disubstituted 3‐hydroxypyrazoles, in contrast to the more common synthesis from β‐ketoesters, which gives 1,3‐disubstituted 5‐hydroxypyrazoles. This reaction is used to prepare several novel pyrazoles bearing haloalkyl substituents. Criteria for assignment of structures have been developed based on physical and spectroscopic properties of the isomers. The regiochemical preference in this addition is considered on the basis of steric, electronic, and mec

ISSN:0022-152X    

DOI:10.1002/jhet.5570300110

出版商:Wiley‐Blackwell    

年代:1993

数据来源: WILEY