3-氨基-1-丙醇置于十二羰基三钌,水,2-(二环己基膦酰基)-1-苯基-1H-吡咯体系中,用 环己烷 作为反应溶剂,化学反应 21.0H,反应生成 杂氮环丁烷 参考文献:Amino-Alcohol Cyclization: Selective Synthesis Of Lactams And Cyclic Amines From Amino-Alcohols 标题:Amino-Alcohol Cyclization: Selective Synthesis Of Lactams And Cyclic Amines From Amino-Alcohols 摘要:通过使用一种原本用于醇与氨直接合成胺的催化剂,可以将n-氨基醇选择性地环化反应生成酰胺或胺.通过添加水,可以反应生成主要产物--胺;而添加供氢受体作为牺牲性酮,则会反应生成主要产物--酰胺.在不添加任何辅助剂的情况下,观测到同时反应生成了胺和酰胺.在这些条件下,N-取代氨基醇仅反应生成环状胺.从2-(N-烷醇)苯胺出发,产生了环状胺,其中n-丙醇衍生物选择性地主要反应生成喹啉. DOI:10.1039/c3Cy00513E
专利号:US-12291596-B2 优先权日:2018-11-30 标 题 :Radical cascade-enabled synthesis of precision polymers with complex main-chain structures 发明人:NIU JIA; HUANG HANCHU; WANG WENQI 权利人:THE TRUSTEES OF BOSTON COLLEGE 摘要:Radical cascade reactions enabling sequence-controlled ring-closing polymerization and ring-opening polymerization for the controlled synthesis of polymers with complex main-chain structures are provided. Facile syntheses leading to low-strain macrocyclic monomers consisting of the ring-opening triggers and extended main-chain structures are also provided. The present disclosure further provides methods for excellent control over polymer molecular weights and molecular weight distributions and high chain-end fidelity allows for the preparation of polymeric systems with well-defined architectures. Further provided are the general nature of the radical cascade-triggered transformations in polymer chemistry, and its application to the synthesis of polymers with diverse main-chain structural motifs with tailored functions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:US-12421534-B2 优先权日:2021-11-10 标 题 :Engineered enzymes and method for the synthesis of diverse tyrosine analogs 发明人:ALMHJELL PATRICK J; ARNOLD FRANCES H 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein is an engineered tryptophan synthase β-subunit (TrpB) that catalyzes the synthesis of tyrosine, tyrosine analogs, or salts thereof. Also provided herein are methods for preparing tyrosine, tyrosine analogs, or a salt thereof using the engineered TrpB described herein.
专利号:US-11161827-B2 优先权日:2019-04-05 标 题 :Catalytic systems for stereoselective synthesis of chiral amines by enantiodivergent radical C—H amination 发明人:Zhang xiao-xiang; Lang kai 权利人:TRUSTEES BOSTON COLLEGE; THE TRUSTEES OF BOSTON COLLEGE 摘要:In one aspect, the disclosure relates to a mode of asymmetric induction in radical processes based on sequential combination of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution. Also disclosed is an asymmetric system for stereoselective synthesis of strained 5-membered cyclic sulfamides via radical 1,5-C—H amination of sulfamoyl azides. The disclosed metalloradical system can control the degree and sense of asymmetric induction in the catalytic radical C—H amination in a systematic manner. The disclosed system is applicable to a broad scope of substrates with different types of C(sp 3 )—H bonds and exhibits reactivity and selectivity, providing access to both enantiomers of useful 5-membered cyclic sulfamides in a highly enantioenriched form. Also disclosed are catalysts useful in these processes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
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-8138346-B2 优先权日:2006-08-16 标题 :Method for synthesis of 8-alkoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones 发明人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG 权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; HASHIMOTO AKIHIRO; WANG QIUPING; LUCIEN EDLAINE; PAIS GODWIN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC 摘要:The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. n nThe substituents R, R 5 , R 6 , R 7 , R 8 and R 9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.