专利号:US-8598346-B2 优先权日:2008-07-16 标 题 :Synthesis of cyclic amidines 发明人:LENTZEN GEORG; NEUHAUS THORSTEN 权利人:LENTZEN GEORG; NEUHAUS THORSTEN; BITOP AG 摘要:The invention relates to an innovative method for synthesis of cyclic amidines. The synthesis starts from a β-, γ- or δ-lactone which is twofold brominated. After esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. The ring closure to the cyclic amidine is accomplished subsequently by reaction with orthoester, imidate or thioimidate. Owing to interposing additional steps for recovery of the diamino compound in enantiomerically pure form, the enantiomers of the cyclic amidines can be stereoselectively synthesized.
专利号:EP-2883866-A1 优先权日:2012-08-13 标题 :INTERMEDIATE FOR SYNTHESIS OF 1-(2-DEOXY-2-FLUORO-4-THIO-beta-D-ARABINOFURANOSYL) CYTOSINE, INTERMEDIATE FOR SYNTHESIS OF THIONUCLEOSIDE, AND METHODS FOR PRODUCING THESE INTERMEDIATES
专利号:WO-2014027658-A1 优先权日:2012-08-13 标题 :INTERMEDIATE FOR SYNTHESIS OF 1-(2-DEOXY-2-FLUORO-4-THIO-β-D-ARABINOFURANOSYL) CYTOSINE, INTERMEDIATE FOR SYNTHESIS OF THIONUCLEOSIDE, AND METHODS FOR PRODUCING THESE INTERMEDIATES
专利号:MX-2015001935-A 优先权日:2012-08-13 标 题 :INTERMEDIARY FOR SYNTHESIS OF 1- (2-DEOXI-2-FLUORO-4-TIO-BETA-D-A RABINOFURANOSIL) CITOSINE, INTERMEDIARY FOR SYNTHESIS OF TIONUCLEOSIDE AND METHODS TO PRODUCE THESE INTERMEDIARIES.
专利号:ES-2718307-T3 优先权日:2012-08-13 标题 :Intermediate for the synthesis of 1- (2-deoxy-2-fluoro-4-thio-beta-d-arabinofuranosyl) cytosine, intermediate for the synthesis of thionucleoside and methods to produce these intermediates
专利号:US-6028224-A 优先权日:1998-06-22 标 题 :Fluoxetine process from benzoylpropionic acid 发明人:HILBORN JAMES WALLACE; JURGENS ALEX ROGER; SENANAYAKE CHRIS HUGH 权利人:SEPRACOR INC 摘要:A synthesis of fluoxetine is disclosed. The process begins with a lower alkyl ester of 3-benzoylpropionic acid, which is reduced in the presence of a chiral ligand to produce the corresponding γ-hydroxy ester, and the ester is cleaved. The free acid is then condensed with the alcohol to form a γ-lactone, which is treated with ammonia to provide the γ-hydroxy amide. The amide undergoes a Hoffman rearrangement to provide a 2-oxo-1,3 oxazine, which is reduced to 3-(methylamino)-1-phenyl-1-propanol. The alcohol is deprotonated and reacted with a 4-chloro- or 4-fluoro benzotrifluoride to provide fluoxetine free base.
参考标题:Synthesis Of Cyclic Amidines 摘要:The Invention Relates To An Innovative Method For Synthesis Of Cyclic Amidines. The Synthesis Starts From A β-, γ- Or δ-Lactone Which Is Twofold Brominated. After Esterification Of The Carboxyl Function, The Bromine Atoms Are Nucleophilically Substituted And The Corresponding Diamino Compound Is Obtained. The Ring Closure To The Cyclic Amidine Is Accomplished Subsequently By Reaction With Orthoester, Imidate Or Thioimidate. Owing To Interposing Additional Steps For Recovery Of The Diamino Compound In Enantiomerically Pure Form, The Enantiomers Of The Cyclic Amidines Can Be Stereoselectively Synthesized.
合成参考文献
参考文献:10.1515/znc-2005-9-1019 摘要:Wood WF, Walsh A, Seyjagat J, Weldon PJ. Volatile compounds in shoulder gland secretions of male flying foxes, genus Pteropus (Pteropodidae, Chiroptera). Z Naturforsch C J Biosci. 2005 Sep;60(9-10):779–84. doi: 10.1515/znc-2005-9-1019.