摘要:

AbstractIndole‐3‐carboxylic acid (as well as indole‐3‐glyoxylic acid) derivatives are readily prepared from indoles (including oxindoles) and phosgene (oxalyl chloride), respectively. The interaction of these reagents with the indole Grignard reagent afforded several products including the cyclo‐tetramers,21and30. Indolo‐fused heterocycles can be readily prepared from the reaction of phosgene (or oxalyl chloride) with suitable reactants. Thuse.g., phosgene and 2‐(2‐hydroxy‐phenyl)‐N‐methylindole readily gave 5,6‐dihydro‐11‐methyl‐6‐oxobe

ISSN:0022-152X    

DOI:10.1002/jhet.5570140701

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

AbstractOxidation of 4‐[3‐(dimethylamino)propyl]‐3,4‐dihydro‐2‐(1‐hydroxyethyl)‐3‐phenyl‐2H‐1,4‐benzothiazine, hydrochloride (I) with hydrogen peroxide yielded a mixture of two sulfoxides (II). Since this mixture exhibited antiinflammatory activity, the two components (Isomers A and B) were prepared in purified form by oxidation of I withN‐chlorosuccinimide and hydrogen peroxide, respectively. Isomer A was more potent than Isomer B in the carra

ISSN:0022-152X    

DOI:10.1002/jhet.5570140702

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

AbstractSynthetic routes leading to the preparation of 4‐substituted 1,4‐benzodiazepine‐3,5‐diones are described. Thus, 2‐carbobenzoxyaminobenzoic acid was converted to itsp‐nitrobenzyl ester (I) and the decarbobenzoxylated product (II) gave, with ethyl α‐bromoacetate,N‐(2‐carboxyp‐nitrobenzylate)phenylglycine ethyl ester (III). The latter was hydrogenolyzed toN‐(2‐car‐boxy)phenylglycine ethyl ester (IV), which was coupled with benzylamine to giveN‐(2‐carboxy‐benzylamido)phenylglycine ethyl ester (VIa). Saponification of VIa affordedN‐(2‐carboxy‐benzylamido)phenylglycine (VIIa) which was cyclized with DCCI to produce 4‐benzyl‐2H‐1,4‐benzodiazepine‐3,5(lH,4H)dione (VIIIa). Alternatively, 2‐nitro‐N‐phenylbenzamide (Xb) was reduced to 2‐amino‐N‐phenylbenzamide (XIb) which was converted toN‐(2‐carboxanih'do)‐phenylglycine ethyl ester (VIb). The latter was converted to 4‐phenyl‐2H‐1,4‐benzodia

ISSN:0022-152X    

DOI:10.1002/jhet.5570140703

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

AbstractA general method is described for the synthesis of 2‐amino‐3‐carbethoxy‐l‐hydroxyindoles by the reductive cyclization of 2‐nitrophenylcyanoacetates using zinc and acetic acid at temperature

ISSN:0022-152X    

DOI:10.1002/jhet.5570140704

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

AbstractThe title compound (14), a representative of a novel ring system, was prepared from 9H‐carbazole‐1‐carboxylic acid 1‐methylhydrazide (7) and triethyl orthoformate. Attempted cyclization of7with triethyl orthoacetate led only to 9H‐carbazole‐l‐carboxylic acid 2‐(l‐ethoxyethylidene)‐l‐methylhydrazide (16). Treatment of16with trifluoroacetic acid gave 9H‐carbazole‐1‐carboxylic acid (12). A postulated mechanism for this transformation was supported by studies with model compounds. A new synthesis of1‐benzoyl‐2‐methylhydrazine (24), using 1‐acetyl‐1‐methylhy

ISSN:0022-152X    

DOI:10.1002/jhet.5570140705

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

AbstractThe preparation of 2,4,6‐trinitrophenyl (picryl) derivatives of triazine, pyrimidine, thiophene, furan, thiazole, 1,3,4‐oxadiazole and 1,3,4‐thiadiazole is described. The picryl derivatives are prepared by the Ullmann reaction and by cyclization reactions to form the heterocyclic

ISSN:0022-152X    

DOI:10.1002/jhet.5570140706

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

AbstractThe scope of the nucleophilic displacement of aromatic halogens on 1,4‐benzodiazepine precursors by the anions of pyrroles, pyrazoles and imidazoles was studied both with and without electron‐withdrawing substitutents on the heterocyclic nucleophiles. Some of the products proved to be useful intermediates for the synthesis of novel fused 1,4‐benzodiaze

ISSN:0022-152X    

DOI:10.1002/jhet.5570140707

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

AbstractThe syntheses of novel 8‐chloropyrazolo[1,5‐a][1,4]benzodiazepines and of an imidazo‐benzodiazepinone utilizing products from the nucleophilic substitution of fluorine in 2‐fluoro‐5‐nitrobenzophenone (1) by pyrazole‐3,5‐dicarboxylic acid, dimethyl ester (2) and by 2‐methyl‐imidazole‐4,5‐dicarboxylic acid, diethyl e

ISSN:0022-152X    

DOI:10.1002/jhet.5570140708

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

AbstractThe preparation of 8‐nitro substituted pyrazolobenzodiazepines from 2‐fluoro‐5‐nitrobenzo‐phenone (1) and 3,5‐diacetoxymethylpyrazole (2)

ISSN:0022-152X    

DOI:10.1002/jhet.5570140709

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY

摘要:

Abstract1H‐ and 2H‐Pyrazolo[3,4‐f]quinolines were synthesized in order to get an antibacterial compound by two different methods from 6‐nitro‐ and 6‐am

ISSN:0022-152X    

DOI:10.1002/jhet.5570140710

出版商:Wiley‐Blackwell    

年代:1977

数据来源: WILEY