CAS: 351862-32-3; (R)-1-(Chroman-2-yl)-N-((5-(4-Fluorophenyl)Pyridin-3-yl)Methyl)Methanamine

📜色酮 在 吡啶,三乙基硅烷,二甲基十二/十四烷基叔胺,三氟甲磺酸,C29H40N4O4,对甲苯磺酸,三乙胺,Cerium Triflate体系中,用 二氯甲烷,甲苯作为反应溶剂,反应 40.0H,获得 Sarizotan
参考文献:氰化物与色酮和β-取代环己酮的不对称催化共轭加成
标题:氰化物与色酮和β-取代环己酮的不对称催化共轭加成
摘要:通过手性路易斯酸和非手性有机碱的双重催化,实现了环状 α,β-不饱和酮的高度对映选择性共轭氰化.多种色酮和β-取代的环己烯酮在温和条件下以高对映选择性高收率转化为所需的β-氰基酮衍生物.金属盐 Ce(Otf) 3和 Ba(Otf) 2与手性n,N '-二氧化物的结合很好地促进了反应,揭示了反应结果与路易斯酸度与金属离子半径之间的密切联系.生物活性化合物 Repinotan 和 Sarizotan 的轻松合成突出了这些方法的应用.
Doi:10.1021/Acscatal.2C05509

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:WO-2009094569-A2
优先权日:2008-01-25
标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

专利号:US-2005222431-A1
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

专利号:US-7227028-B2
优先权日:2003-12-30
标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

专利号:US-2007244331-A1
优先权日:2003-12-30
标 题 :Synthesis of Acyloxyalkyl Carbamate Prodrugs and Intermediates Thereof