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71.
Max Robba Daniel Maume Jean-Charles Lancelot 《Journal of heterocyclic chemistry》1978,15(7):1209-1213
Electrophilic substitution reactions of the 1- and 4-triazino-indolones were made on lactamic nitrogen with methyl sulphate or benzyl chloride and on the homocycle with bromine or nitric acid. BrominatJon and nitration reactions gave either mono-substitutions on position 10 or disubstitutions on position 7 and 10 or 9 and 10 or polysubstitutions leading to mixtures of tri-and tetrasubstituted compounds. The structure of the derivatives was determined by nmr, study of the NOE effect and unequivocal synthesis. 相似文献
72.
Bertrand Letois Jean Charles Lancelot Carmela Saturnino Max Robba Paolo De Caprariis 《Journal of heterocyclic chemistry》1992,29(7):1769-1772
A series of trans-thienyl-3-ethoxycarbonyl-2,3-dihydro[1,5]benzothiazepin-4(5H)-ones 6-8 was synthesized from thienylmethylidenemalonates 3a-3c and 2-aminobenzenethiol 3d in the presence of triethylamine hydrochloride at 160°. The [1,5]benzothiazepines 6-8 were alkylated using 2-dimethylaminochloroethane, 3-dimethylaminochloropropane and 3-(N-piperidino)chloropropane in order to obtain the corresponding 5-aminoalkylbenzothiazepinones 9-14 . 相似文献
73.
A facile synthetic route to the new 2-TIPS-oxazol-5-ylboronic acid pinacol ester was described herein. Its reactivity toward Suzuki cross-coupling reaction was studied to provide various 5-(het)aryloxazoles. A wide range of functions on the aryl moiety are tolerated. 相似文献
74.
75.
Bureau R Daveu C Lemaître S Dauphin F Landelle H Lancelot JC Rault S 《Journal of chemical information and computer sciences》2002,42(4):962-967
A definition of a pharmacophore for the 5-HT4 antagonist was carried out by considering a three-dimensional model which correlates the chemical structures of series of antagonists with their biological affinities. A molecular design is described by analyzing the differences between two 3D serotonin pharmacophores. This successful structural modification demonstrates the efficiency of this approach to design new serotonin ligands. 相似文献
76.
François-Xavier Le FoulonEmmanuelle Braud Frédéric FabisJean-Charles Lancelot Sylvain Rault 《Tetrahedron》2003,59(50):10051-10057
This paper describes a general procedure for the synthesis of new substituted thiaisatoic anhydrides or 6- or 7-aryl-1H-thiéno[3,2-d][1,3]oxazine-2,4-diones 3a-j and 4a-f. They were synthesized in large scale under microwave heating conditions with high yields. The reactivity vs nucleophilic reagents of these compounds was studied and permitted to develop a simple combinatorial procedure to synthesize a library of new thiophene ureidoacids 7a-j and 8a-j. 相似文献
77.
78.
Yamien Effi Sylvain Rault Jean-Charles Lancelot Max Robba 《Journal of heterocyclic chemistry》1987,24(2):431-435
5-Aminopyrrolo[1,2-a]thieno[2-3-3]pyrazine derivatives were obtained by intramolecular cyclisation of N3(1-pyrrolyl)-2-thienylurea derivaties. Synthesis of these latter compounds was achieved from 2-(1-pyrrolyl)-3-thenoylazide via a curtius rearrangement. The H nmr spectra are discussed. 相似文献
79.
Jean-Marie Gazengel Jean-Charles Lancelot Sylvain Rault Max Robba 《Journal of heterocyclic chemistry》1989,26(4):1135-1139
The synthesis of dihydropyrimidinocarbazoles 12,15 and 18 was achieved by cyclization of tetrahydrocarbazolones with triformamidomethane. The oxidation with potassium permanaganate of dihydropyrimidinocarbazoles gave the pyrimidinocarbazoles 13,16 and 19. The application of the Sandemeyer reaction to amiononitrocarbazoles gave cyanonitrocarbazoles which could be reduced to aminocyanocarbazoles 1 and 7. Intramolecular cyclization of the carbazoles 1 and 7 afforded 3,4-dilhydro-4-oxo-6H-pyrimidino[5,4-b]carbazole 2 and 1,2-dighydro-1-oxo-6H-pyrimidino[5,4-b]carbazole 10 was obtained by cyclization of quinazolinyl hydrazone 9 with hydrochloric acid and acetic acid. The structure of the derivatives was determined by 1H-nmr and the Overhauser effect. 相似文献
80.
Saturnino C Capasso A Lancelot JC Rault S Buonerba M De Martino G 《Chemical & pharmaceutical bulletin》2002,50(9):1151-1154
Seven morpholin derivatives were synthesized (compounds 1-7) and their behavioural effects were evaluated; the elements considered were locomotor activity, motor coordination, catalepsy, stereotyped behaviour and antinociception. All the compounds, at doses of 10-20-40 mg/kg/i.p., induced a reduction of all behavioural elements without a significant antinociceptive effect. These results indicate that these morpholin derivatives affect the central nervous system. 相似文献