A silodosin intermediate and its preparation method, and the intermediate for method of preparation of the silodosin
The invention relates to the field of compound synthesis and especially relates to a silodosin intermediate, a preparation method of the silodosin intermediate, and a method for preparing silodosin from the silodosin intermediate. The method for preparing silodosin from the silodosin intermediate has the characteristics of economy, safety, high purity and high yield and is suitable for large-scale industrial production.
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(2017/08/26)
Process for producing 5-methylindolines
Presentation of a method for producing a 5-methylindoline represented by the formula: STR1 (wherein R is a hydrogen atom or a lower alkyl group), which comprises catalytically hydrogenating a 1-(substituted)benzyl-5-formylindoline represented by the formula: STR2 (wherein R1 is a hydrogen atom or a lower alkyl group, and R2 is a hydrogen atom, a lower alkyl group or a lower alkoxy group) in the presence of an inert solvent and a palladium catalyst.
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(2008/06/13)
Tyrphostins. 2. Heterocyclic and α-Substituted Benzylidenemalonitrile Tyrphostins as Potent Inhibitors of EGF Receptor and ErbB2/neu Tyrosine Kinases
We have previously described a novel series of low molecular weight protein tyrosine kinase inhibitors which we named tyrphostins.The characteristic active pharmacophore of these compounds was the hydroxy-cis-benzylidenemalonitrile moiety.In this article we describe three novel groups of tyrphostins: (i) one group has the phenolic moiety of the cis-benzylidenemalononitrile replaced either with other substituted benzenes or with heteroaromatic rings, (ii) another is a series of conformationally constrained derivatives of hydroxy-cis-benzylidenemalononitriles in which the malononitrile moiety is fixed relative to the aromatic ring, and (iii) two groups of compounds in which the position trans to the benzenemalononitrile has been substituted by ketones and amides.Among the novel tyrphostins examined we found inhibitors which discriminate between the highly homologous EGF receptor kinase (HER1) and ErbB2/neu kinase (HER2).These findings may lead to selective tyrosine kinase blockers for the treatment of diseases in which ErbB2/neu is involved.
Selective monoamine oxidase inhibitors. 3. Cyclic compounds related to 4-aminophenethylamine. Preparation and neuron-selective action of some 5-(2-aminoethyl)-2,3-dihydroindoles
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Florvall,Kumar,Ask,Fagervall,Renyi,Ross
p. 1406 - 1412
(2007/10/02)
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