On September 20, 2007, Alcaraz, Lilian; Lister, Andrew; Pairaudeau, Garry published a patent.Product Details of 142327-44-4 The title of the patent was Preparation of aminohydroxyethylbenzothiazolones as β2 adrenoreceptor agonists. And the patent contained the following:
Title compounds ArCH(OH)CH2NHC(R1)(R2)TAXYWCR51R52NR3R4 [I Ar = 4-hydroxy-2-oxo-3H-1,3-benzothiazol-7-yl; T = a bond, CR33R34, CR35R36CR37R38, CR39R40CR41R42CR43R44; W = a bond, CR45R46, CR47R48CR49R50; A = a bond, (un)substituted (hetero)aryl; X = a bond; Y = a bond, (un)substituted (hetero)aryl; but A and Y not both a bond; R3, R4 = independently H, (un)substituted alkyl, heterocyclyl, cycloalkyl; or R3NR4 = (un)substituted 4-12 membered monocyclyl or bicyclyl; R33-R50 = independently H, alkyl; and their pharmaceutically acceptable salts], (e.g., II•2TFA), were prepared as β2 adrenoreceptor agonists. Thus, a multi-step synthesis from Et 2-(3-methylphenyl)acetate was given for benzothiazolone salt II•2TFA. Selected I were tested for adrenergic β2 mediated cAMP production Certain benzothiazolones I were at least 10-fold more potent at the β2 receptor compared to the α1, β1, or dopamine (D2) as demonstrated by selectivity assays. I, and their pharmaceutical compositions, are useful for the treatment of diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Product Details of 142327-44-4
The Article related to aminohydroxyethylbenzothiazolone preparation beta2 adrenoreceptor agonist respiratory disease, benzothiazolone hydroxy aminohydroxyethyl preparation beta2 adrenoreceptor agonist and other aspects.Product Details of 142327-44-4
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