PROCEDIMIENTO DE SINTESIS Y FORMA CRISTALINA HIDROCLORURO DE 4-{3-[CIS-HEXAHIDROCICLOPENTA[C]PIRROL-2(1H)-IL]PROPOXI}BENZAMIDA ASI COMO LAS COMPOSICIONES FARMACEUTICAS QUE LA CONTIENEN
ROBERT, NICOLAS,LECOUVE, JEAN-PIERRE,MEUNIER, LOIC,BOIRET, MATHEIU,LERESTIF, JEAN-MICHEL,GAILLARD, MARINA,LETELLIER, PHILIPPE
申请号：
PE0006952012
公开号：
PE00462013A1
申请日:
2012.05.22
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
Refers to a procedure for the synthesis of the compound of formula (i), which comprises: a) reacting a compound of formula (ii) with Ammonia at a higher temperature to 100C to form the compound of formula (iii) (b) Reducing the previous compound in the presence of a catalyst and H M Etalico to give place to the biciclica Amine of formula (iv) (c) The Compound of formula (iv) undergoes(i) a coupling reaction in the presence of an Amine or a Carbonate, Hydroxide, in a Polar Environment constituted by ketones, ethers, among others with a compound of formula (V), where y is - CH2 - HAL HAL is Halogen, among others (ii) an aminative reduction in acid Medium with a Compound of fo Formula (v\u00b4), where r\u00b4\u00b4 ry are independently alkyl - (C1 - C6)Among others or (iii) a Reductive amination with a compound of formula (v\u00b4\u00b4), giving rise to the Free Base of the compound of formula (i) in the presence of hydrochloric acid is the compound of formula (i).Also refers to a Crystalline form characterized by a diagram of X diffraction on Powder diffraction Lines (Bragg Angle 2 - Theta -): 16,97\u00ba, 17,84\u00ba 18,90\u00ba, 20,32\u00ba 23,87\u00ba, 27,10\u00ba, 27,86\u00ba and 30,34\u00ba. Also referred to as a Pharmaceutical composition, useful for the treatment of cognitive disorders and psicocomportamentalesSE REFIERE A UN PROCEDIMIENTO DE SINTESIS DEL COMPUESTO DE FORMULA (I) QUE COMPRENDE: A) HACER REACCIONAR EL COMPUESTO DE FORMULA (II) CON AMONIACO A UNA TEMPERATURA SUPERIOR A 100ºC PARA FORMAR EL COMPUESTO DE FORMULA (III) B) REDUCIR EL COMPUESTO ANTERIOR EN PRESENCIA DE H Y DE UN CATALIZADOR METALICO PARA DAR LUGAR A LA AMINA BICICLICA DE FORMULA (IV) C) EL COMPUESTO DE FORMULA (IV) SE SOMETE A: i) UNA REACCION DE ACOPLAMIENTO EN PRESENCIA DE UN CARBONATO, AMINA O UN HIDROXIDO, EN UN MEDIO POLAR CONSTITUIDO POR CETONAS, ETERES, ENTRE OTROS CON UN COMPUESTO DE FORMULA (V), DONDE Y ES -CH2-HAL, HAL ES HALOGENO, ENTRE OTROS ii) UNA AMINACION REDUCTORA EN
