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Process for the preparation of a PDE4 inhibitor
专利权人:
CHIESI FARMACEUTICI S.P.A.
发明人:
ALESSANDRO FALCHI,EMILIO LUTERO,EMANUELE FERRARI,FAUSTO PIVETTI,ROCCO BUSSOLATI,EDOARDO MARIANI,ORSOLA VECCHI,ERHARD BAPPERT,CATERINA VENTRICI
申请号:
ARP140103938
公开号:
AR098128A1
申请日:
2014.10.20
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
1. The formulation and process of the compound with phosphotriase inhibitor activity (PDE4) (1); It also relates to the crystallization and insulation process of formula compound (1) and its application in the production of agroforestry compounds.Inhalation agents used in combination with appropriate means of transport or vehicles. The synthetic products are suitable for medical applications, such as the treatment of respiratory diseases. They also claim that for formula compounds (3)(4) and (5). Claim 1: A process for preparing a compound of formula (1) wherein n is 0 or 1, characterized in that said process comprises: a) reacting a compound of formula (2) where n is 0 or 1, with a compound of formula (3) wherein X is selected from -NHSO₂Me and -NO₂ and Z is selected from -OH, chlorine, bromine, C₁₋₆ linear or branched alkoxy, aryloxy, arylalkoxy, C₁₋₆ alkylcarbonyloxy, arylcarbonyloxy and aryl-C₁₋₆ alkylcarbonyloxy to obtain a compound of formula (1) wherein n is 0 or 1 or a compound of formula (4) where n has the meanings indicated above and X is -NO₂;And, when a formula compound (4) is obtained in step (a), (b) is reduced to the corresponding formula compound (5) whose n is 0 or 1, and reacts with the halothiomethane to obtain a formula compound (1), wherein n has the above meaning; The equation compound (2) in step (a) is obtained from the oxidation of an equation compound (6) by any of the following alternative steps (C1) or C2, where n is 0 or 1 to obtain an equation compound (7) and N is 0 or 1,And subsequent corresponding ion reduction to obtain a formula compound (2), wherein n has the above meaning; or (2) separation of a formula compound (6) by chromatography, wherein n is 0 or 1, 1. To obtain a compound of formula (2) and formula (8), the meaning of which is as above; Alternatively, the formula compound (8) obtained in step C2 may be oxidized to the corresponding formula compound (7) and then reduced to a formula compound (6), which in the chromatograph
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