专利号:WO-2023151188-A1 优先权日:2022-02-08 标题 :Green synthesis method of antiviral drug intermediate 发明人:XIA BIN; WANG JIAMING; ZHANG XIANSHU; CAI LINGLI; WANG ZIKUN; CAO MING; YANG SHAOBO; GAO QIANG; ZHENG BAOFU 权利人:SHANGHAI HAOYUAN CHEMEXPRESS CO LTD 摘要:The present application provides a green synthesis method of an antiviral drug intermediate. The method comprises: in the presence of a catalyst, adding zinc powder into a compound as represented by a formula II and performing a cyclization reaction with dihaloalkane to generate a compound as represented by a formula I, zinc halide being not required to be added to the cyclization reaction, wherein R1 is selected from H or an amino-protecting group, and R2 is selected from substituted or unsubstituted C1-C10 alkyl, substituted or unsubstituted C6-C14 aryl or substituted or unsubstituted C7-C14 aralkyl; R3 and R4 are each independently selected from hydrogen, substituted or unsubstituted C1-C10 alkyl, and R3 and R4 can be connected to form a fatty ring containing 3-10 carbon atoms. The synthesis method is short in steps, dangerous and expensive materials are not used, a reaction conversion rate is high, reaction time is short, and operation is easy and convenient. Production costs and post-treatment costs are reduced, and a cost advantage is obvious. The method can be widely used for preparing antiviral drugs of nirmatrelvir, boceprevir or narlaprevir, and has good market prospects.
专利号:EP-1919850-B1 优先权日:2005-08-11 标题:Nitro substituted alpha-olefin synthesis catalysts 发明人:ADELMAN DOUGLAS J; IONKIN ALEX SEREGY 权利人:DU PONT 摘要:Iron, cobalt, chromium or vanadium complexes of 2,6-pyridinedicarboxaldehydes diimines and 2,6-diacylpyridines diimines which are suitable for catalyzing the oligomerization of ethylene to alpha-olefins exhibit more prolonged catalytic activity if aryl groups attached to the imino carbon atom(s) are substituted with at least one nitro group.