Improvements in the subject-matter of patent of invention No. 529,608 relating to "process for obtaining new 1H- imidazole derivatives"

• Format: Patent
• Language: English; Spanish
• Published: 16.02.1986
• Edition: 4
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

Process for obtaining 1H-imidazole derivatives of general formula I": comprising the reaction of a compound of formula II where A is methine (-CH-) with a compound of formula III" where X is bromine or chlorine, R"' is a halogen atom selected from chlorine or fluorine in any of the 5 or 7 positions of the benzo[b]thiophene residue and joining the methylene group (-CH2-) to the benzo[b]thiophene residue in the 2 or 3 position thereof, in hexamethyl phosphorotriamide, in the presence of a mineral base, preferably sodium hydride, and at a temperature of between 0 degree C and 100 degree C for a period of time of between 1 and 24 hours, with purification by crystallization or extraction, washing, drying and chromatography, yielding addition salts by treatment with the corresponding acids. Process for obtaining 1H-imidazole derivatives of general formula I": comprising the reaction of a compound of formula II where A is methine (-CH-) with a compound of formula III" where X is bromine or chlorine, R"' is a halogen atom selected from chlorine or fluorine in any of the 5 or 7 positions of the benzo[b]thiophene residue and joining the methylene group (-CH2-) to the benzo[b]thiophene residue in the 2 or 3 position thereof, in hexamethyl phosphorotriamide, in the presence of a mineral base, preferably sodium hydride, and at a temperature of between 0 degree C and 100 degree C for a period of time of between 1 and 24 hours, with purification by crystallization or extraction, washing, drying and chromatography, yielding addition salts by treatment with the corresponding acids. < IMAGE > MEJORAS EN EL OBJETO DE LA PATENTE DE INVENCION NUM. 529.608 QUE SE REFIERE A PROCEDIMIENTO DE OBTENCION DE NUEVOS DERIVADOS DEL 1H-IMIDAZOL. CONSISTE EN: A) HACER REACCIONAR UN COMPUESTO DE FORMULA (II) CON UN COMPUESTO DE FORMULA (III), EN UN DISOLVENTE APROTICO, COMO HEXAMETILFOSFOROTRIAMINA, EN PRESENCIA DE UNA BASE MINERAL, COMO HIDRURO SODICO, A UNA TEMPERATURA DE 0 A 100JC, DURANTE 1 A 24 HORAS, PARA OBTENER UN COMPUESTO DE FORMULA (I) Y SUS SALES NO TOXICAS FARMACEUTICAMENTE ACEPTABLES, PREFERENTEMENTE MONONITRATOS; Y B) PURIFICAR POR CRISTALIZACION; EXTRACCION; LAVADO CON AGUA, SECADO Y CROMATROGRAFIA DE COLU