[EN] PI-3 KINASE INHIBITOR PRODRUGS<br/>[FR] PROMEDICAMENTS D'INHIBITEURS DE PI-3 KINASE
申请人:SEMAFORE PHARMACEUTICALS INC
公开号:WO2004089925A1
公开(公告)日:2004-10-21
The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
Nucleophilic addition-elimination reactions of N-(p-tolylsulphonyl)vinylsulphoximines: preparation of α-methylene nitriles and phosphonates
作者:Peter L. Bailey、Richard F.W. Jackson
DOI:10.1016/0040-4039(91)80705-b
日期:1991.6
Treatment of N-(p-tolylsulphonyl)vinylsulphoximines (1) with lithium cyanide in DMF at room temperature leads to efficient formation of α,β-unsaturated nitriles (3), via a Michael addition-proton transfer-elimination process, in which the polarity of the double bond is reversed. Analogous reaction with lithium dimethylphosphonate leads to β-dimethylphosphonyl sulphoximines (7), which are converted
PREPARATION AND TOXICITY OF SOME ALKYL THIOPYROPHOSPHATES
作者:R. A. McIvor、G. D. McCarthy、G. A. Grant
DOI:10.1139/v56-235
日期:1956.12.1
Several methods have been investigated for the synthesis of tetraalkyl thiopyrophosphates, including one that can be carried out very rapidly with high yield. Purification of these compounds proved exceedingly difficult, because they were sensitive to traces of acids or bases, and probably to inorganic salts at temperatures above 70 °C. All methods investigated yield only the thiono isomer, there being
已经研究了几种合成硫代焦磷酸四烷基酯的方法,包括一种可以非常快速且产率高的方法。事实证明,这些化合物的纯化极其困难,因为它们对痕量的酸或碱敏感,并且可能在 70 °C 以上的温度下对无机盐敏感。所有研究的方法仅产生硫代异构体,没有证据表明相应的 P-S-P 异构体。毒理学研究不支持 Fiszer 和工作人员报告的结果。没有一种化合物比焦磷酸四乙酯在静脉内的毒性更大。报道了用于红外研究的几种其他相关化合物的合成。
4-Biarylyl-1-phenylazetidin-2-ones useful for the treatment of hypercholesterolemia are disclosed. The compounds are of a general formula (I) in which formula (II) represents an aryl or heteroaryl residue, Ar represents an aryl residue; U is a two to six atom chain; and the R’s represent substituents.
CRYSTAL OF CYCLIC PHOSPHONIC ACID SODIUM SALT AND METHOD FOR MANUFACTURING SAME
申请人:OTSUKA CHEMICAL CO., LTD.
公开号:US20170233421A1
公开(公告)日:2017-08-17
An object of the present invention is to provide a crystal of a cyclic phosphonic acid sodium salt (2ccPA) with high purity and excellent storage stability and a method for producing the crystal. The present invention provides a crystal of a cyclic phosphonic acid sodium salt (2ccPA) represented by formula (1):