Synthesis of N,N-Dimethyl-2-(tributylstannyl)methyl-5-substituted Benzylamines as a Quinodimethane Precursor by the Reaction of N,N-Dimethyl-N-(tributylstannyl)methyl-4-substituted Benzylammonium Salts with Lithium Diisopropylamide.
作者:Yasuhiro MAEDA、Yoshiro SATO
DOI:10.1248/cpb.46.508
日期:——
Reaction of N, N-dimethyl-N-(tributylstannyl)methyl-4-substituted benzylammonium salts 2 with lithium diisopropylamide (LDA) gave N, N-dimethyl-2-(tributylstannyl)methyl-5-substituted benzylamines 3 as the main products. Treatment of 3 with iodomethane followed by tetrabutylammonium fluoride (TBAF) in the presence of dimethyl fumarate gave the corresponding dimethyl trans-1, 2, 3, 4-tetrahydro-6-substituted naphthalene-2, 3-dicarboxylates 15 in good yields.
N, N-二甲基-N-(三丁基锡)甲基-4-取代苄基铵盐 2 与二异丙基酰胺锂(LDA)反应,得到主要产物 N, N-二甲基-2-(三丁基锡)甲基-5-取代苄胺 3。用碘甲烷处理 3,然后在富马酸二甲酯存在下用四丁基氟化铵(TBAF)处理,可以得到相应的反式-1,2,3,4-四氢-6-取代萘-2,3-二甲酸二甲酯 15,收率很高。
INHIBITORS OF p38
申请人:Bemis Guy W.
公开号:US20110281878A1
公开(公告)日:2011-11-17
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
[EN] PYRIMIDO-HETEROCYCLIC COMPOUNDS, AND PREPARATION METHOD THEREFOR AND USE THEREOF<br/>[FR] COMPOSÉS PYRIMIDO-HÉTÉROCYCLIQUES, ET LEUR PROCÉDÉ DE PRÉPARATION ET LEUR UTILISATION<br/>[ZH] 一类嘧啶并杂环类化合物、制备方法和用途
The present invention relates to inhibitors (ia)-(id) of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders. All substituents are as in claim 1.
The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.