专利号:US-2012302756-A1 优先权日:2010-02-19 标 题 :Process for synthesis of 2-substituted pyrrolidines and piperadines 发明人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 权利人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 摘要:The present invention provides a highly efficient, versatile one-step process for asymmetric synthesis of either diastereomer of 2-substituted pyrrolidines from a single starting material with excellent yields and high diastereoselectivety. Also provided is a method for the asymmetric synthesis of both diastereomers of 2-substituted piperidines with good yields and excellent diastereoselectivety. Diasteroselectivity is controlled effectively by choice of reducing agent.
专利号:US-2023174567-A1 优先权日:2020-05-22 标题:Synthesis of fluorinated nucleotides 发明人:ARMIGER TRAVIS; BELYK KEVIN M; BENKOVICS TAMAS; CHUNG CHEOL K; JI CHEN YINING; JOHNSON HEATHER CLAIRE; KLAPARS ARTIS; LIU ZHIJIAN; LIU ZHUQING; MOORE JEFFREY C; NEEL ANDREW J; PENG FENG; RUMMELT STEPHAN M; SALEHI MARZUARANI NASTARAN; SHERRY BENJAMIN D; SONG ZHIGUO JAKE; TURNBULL BEN WILLIAM HULME; WANG LU; XU FENG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3′-fluoro-thio-guanosine monophosphate or 3′-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. (I)
专利号:US-6660856-B2 优先权日:2002-03-08 标题 :Synthesis of pyrrolo[2,1-c][1,4]benzodiazepine analogues 发明人:WANG JEH-JENG 权利人:UNIV KAOHSIUNG MEDICAL 摘要:The present invention provides an efficient process for the preparation of pyrrolo [2,1-c][1,4]benzodiazepines (PBDs) represented by the formula (I): n which starts from a subsituted 2-amino benzoic acid compound, and involves a step of an intermediate MOM-protected dilactam compound in the presence of LiBH 4 . The process enables a practital and large scale (e.g. ca. 10 g) synthesis of PBD analogue.
专利号:US-9981935-B2 优先权日:2013-07-05 标 题:Formation of chiral 4-chromanones using chiral pyrrolidines in the presence of acids 发明人:MEDLOCK JONATHAN ALAN; LETINOIS ULLA; NETSCHER THOMAS; BONRATH WERNER 权利人:DSM IP ASSETS BV 摘要:The present invention relates to a synthesis of chromanones or chromanes in a stereospecific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of a specific type and of at least one Bransted acid or in the presence a specific chiral compound having a Bransted acid functional group in the molecule.
专利号:US-9815809-B2 优先权日:2013-07-05 标题:Formation of chiral 4-chromanones using chiral pyrrolidines in the presence of phenols or thiophenols 发明人:LETINOIS ULLA; NETSCHER THOMAS 权利人:DSM IP ASSETS BV 摘要:The present invention relates to a synthesis of chromanones or chromanes in a stereospecific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of formula of a specific type and of at least one phenol or thiophenol.
专利号:US-9809565-B2 优先权日:2013-07-05 标 题 :Formation of chiral 4-chromanones using chiral pyrrolidines in the presence of ureas or thioureas 发明人:LETINOIS ULLA; NETSCHER THOMAS; ACKERMANN STEPHAN 权利人:DSM IP ASSETS BV 摘要:The present invention relates to a synthesis of chromanones or chromanes in a stereospecific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of formula of a specific type and of at least one urea or thiourea.
参考标题:Organocerium Additions To Proline-Derived Hydrazones: Synthesis Of Enantiomerically Enriched Amines 作者:Scott E. Denmark,James P. Edwards,Theodor Weber,David W. Piotrowski |发布日期:2010.5 摘要:The Addition Of Organocerium Reagents (From Both Organolithium And Organomagnesium Precursors) To Chiral Aldehyde Hydrazones Prepared From 1-Aminoproline Derivatives Has Been Studied. The Additions Proceed In Good Yield And High Diastereoselectivity And With Good Nucleophile (Me, N-Bu, I-Pr, T-Bu, Ph, Etc.) And Substrate Scope (Alkyl, Alkenyl And Aryl). The Resulting Hydrazines Can Be Converted To
合成参考文献
摘要:Leipold, F.; Hussain, S.; France, S. P.; Turner, N. J., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 370. 摘要:Leipold, F.; Hussain, S.; France, S. P.; Turner, N. J., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 364. 参考文献:10.1007/s00253-012-4629-4 摘要:Mitsukura K, Kuramoto T, Yoshida T, Kimoto N, Yamamoto H, Nagasawa T. A NADPH-dependent (S)-imine reductase (SIR) from Streptomyces sp. GF3546 for asymmetric synthesis of optically active amines: purification, characterization, gene cloning, and expression. Applied Microbiology and Biotechnology. 2012 Dec 21;97(18):8079–86. doi: 10.1007/s00253-012-4629-4.