Methoxyallene reacts with carbon monoxide in the PdCl2-CuCl2-NaHCO3 (NaHCO3/NaOAc) system in MeOH to afford methyl 2-(dimethoxymethyl)acrylate and 2-chloro-3,3-dimethoxyprop-1-ene; the third product, 2-chloro-1-methoxy-2-propenyl acetate, appears when NaHCO3-NaOAc is used as a buffer component.
The α-dialkoxymethyl α,β-unsaturated ester 1 can be easily converted, under high pressure and at ambient temperature, into the corresponding aza-Michael adducts 2 and/or push–pull α-aminomethyl-β-methoxy-α,β-unsaturated esters 3 by treatment with primary or secondaryamines. The ratio between these two types of products is shown to depend on the nature of the nitrogen nucleophile.
[EN] A METHOD FOR THE PREPARATION OF 2-(4-METHOXYCARBONYLPYRAZOL-L-YL)ADENOSINE AND 2-(4-ETHOXYCARBONYLPYRAZOL-L-YL)ADENOSINE<br/>[FR] PROCÉDÉ DE PRÉPARATION DE LA 2-(4-MÉTHOXYCARBONYLPYRAZOL-L-YL) ADÉNOSINE ET DE LA 2-(4-ÉTHOXYCARBONYLPYRAZOL-L-YL)ADÉNOSINE
申请人:FARMAK A S
公开号:WO2013023626A1
公开(公告)日:2013-02-21
A method for the preparation of 2-(4-methoxycarbonylpyrazol-l-yl)adenosine of formula la and 2-(4-ethoxycarbonylpyrazol-l-yl)adenosine of formula lb by reaction of 2- hydrazinoadenosine of formula III and the sodium salt of 3,3-dimethoxy-2- methoxycarbonylpropen- l-ol of formula Va or the sodium salt of 3,3-diethoxy-2- ethoxycarbonylpropen-l -ol of formula Vb in combination with a solvent and an acidic agent.
METHOD FOR THE PREPARATION OF 2-(4-METHOXYCARBONYLPYRAZOL-1-YL)ADENOSINE AND 2-(4-ETHOXYCARBONYLPYRAZOL-1-YL)ADENOSINE
申请人:Kvapil Lubomir
公开号:US20140206857A1
公开(公告)日:2014-07-24
A method for the preparation of 2-(4-methoxycarbonylpyrazol-1-yl)adenosine of formula 1a and 2-(4-ethoxycarbonylpyrazol-1-yl)adenosine of formula 1b by reaction of 2-hydrazinoadenosine of formula III and the sodium salt of 3,3-dimethoxy-2-methoxycarbonylpropen-1-ol of formula Va or the sodium salt of 3,3-diethoxy-2-ethoxycarbonylpropen-1-ol of formula Vb in combination with a solvent and an acidic agent.
TANAKA M.; ABE Y.; TOKUYAMA K., CHEM. AND PHARM. BULL., 1978, 26, NO 5, 1558-1569
作者:TANAKA M.、 ABE Y.、 TOKUYAMA K.
DOI:——
日期:——
Protein Kinase Inhibitors
申请人:Pharmascience Inc.
公开号:US20170158697A1
公开(公告)日:2017-06-08
The present invention relates to a novel family of protein kinase inhibitors, more specifically the present invention is directed to inhibitors of the members of the Tec or Src protein kinase families. The present invention also relates to processes for the preparation of these compounds, to the pharmaceutical composition comprising them, and to their use in the treatment of proliferative, inflammatory, infectious or autoimmune diseases, disorder or condition in which protein kinase activity is implicated.