Enantioselective reduction of prochiral ketones to optically active secondary alcohols is an important subject in synthetic organic chemistry because the resulting chiral alcohols are extremely useful, biologically active compounds. The new chiral ligands (2R)-2-[benzyl(2-((diphenylphosphanyl)oxy)ethyl)}amino]butyldiphenylphosphinite, 1 and (2R)-2-[benzyl(2-((dicyclohexylphosphanyl)oxy)ethyl)}am
将手性酮对映选择性还原为旋光性仲醇是合成有机化学中的重要课题,因为所得的手性醇是极其有用的生物活性化合物。新的手性配体(2 R)-2- [苄基(2-(((二苯基膦基氧基)乙基)}氨基]丁基二苯基次膦酸酯1和(2 R)-2- [苄基(2-(((二环己基膦基)氧基) )乙基)}氨基]丁基二环己基次膦酸酯2和相应的钌(II)配合物3和4已被制备。这些配合物的结构已通过多核NMR光谱,IR光谱和元素分析的结合得到阐明。31 P– 1 H} NMR,DEPT,1 H– 13 C HETCOR或1 H– 1 H COZY相关性实验用于确认光谱分配。这些钌(II)-次膦酸酯络合物已被用作苯乙酮衍生物不对称转移加氢的催化剂。在最佳条件下,芳族酮以良好的转化率和中等至良好的对映选择性(高达85%ee)降低。
Steroidal esters of the aromatic nitrogen mustard 2-[4-N,N-bis(2-chloroethyl)amino-phenyl]butanoic acid (2-PHE-BU)
作者:Ioanna C. Papaconstantinou、Manolis A. Fousteris、Anna I. Koutsourea、Georgios N. Pairas、Athanasios D. Papageorgiou、Sotiris S. Nikolaropoulos
DOI:10.1097/cad.0b013e328357f687
日期:2013.1
aromatic nitrogen mustard 2-[4-N,N-bis(2-chloroethyl) amino-phenyl]butanoic acid (2-PHE-BU) was synthesized and conjugated with various steroidal alcohols. The resulting steroidal esters were evaluated for their in-vivo toxicity and antileukemicactivity in P388-leukemia-bearing mice. The new derivatives showed significantly reduced toxicity and marginally improved antileukemicactivity compared with free
[EN] INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL<br/>[FR] INHIBITEURS DU CANAL POTASSIQUE MÉDULLAIRE EXTERNE RÉNAL
申请人:MERCK SHARP & DOHME
公开号:WO2013028474A1
公开(公告)日:2013-02-28
The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
with butyllithium resulted in deprotonation at C3 to afford the corresponding organolithium species. These compounds could be trapped with a variety of electrophiles to give products in high yield. Some limitations to the processes chiefly based on steric effects were uncovered. Interesting and potentially useful side reactions were also established. Treatment of benzothiazines 3 and 8 with butyllithium