📜4-(叠氮甲基)苯甲腈置于palladium On Activated Charcoal 盐酸,氨,氢气体系中,用 甲醇,氯仿 作为反应溶剂,化学反应生成 4-氨甲基苄眯二盐酸盐
参考文献:Design,Synthesis,And Evaluation Of Oxyanion-Hole Selective Inhibitor Substituents For The S1 Subsite Of Factor Xa
标题:Design,Synthesis,And Evaluation Of Oxyanion-Hole Selective Inhibitor Substituents For The S1 Subsite Of Factor Xa
摘要:We Have Designed,Synthesized,And Evaluated The Factor Xa Inhibitory Activities Of P-Amidinophenyl-Sulfones,Amines,And Alcohols Intended To Take Advantage Of The Polarity And Hydrogen-Bonding Potential Of The Oxyanion Hole Region Of The S1 Specificity Pocket. We Demonstrate That Placement Of An Anionic Group Within The Oxyanion Bole Region Of The Catalytic Site Substantially Enhances Activity,With Small Flexible Groups Favored Over Bulkier Ones. Ab Initio Pk(A) Calculations Suggest That The Hydroxyl Substituent Frequently Used For Benzamidine Moieties May Be Ionized To Form An Anionic Group,Consistent With The General Trend. One Nonamidine Based Substituent Also Shows Promising Activity. (C) 2004 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2004.07.054