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  • Copper-Catalyzed Electrophilic Amination of Organoboron Compounds
    [作者:LALIC GOJKO; RUCKER RICHARD P,期刊:SYNLETT, 页码:269-275 , 文章类型: Article,,卷期:2013年-3]
  • A new procedure for direct transformation of alkenes to tertiary alkylamines based on hydroboration and copper-catalyzed amination of alkylboranes is described. The new method is presented in a broader context provided b...
  • Stereoselective Organocatalytic Alkylations with Carbenium Ions
    [作者:GUALANDI ANDREA; COZZI PIER GIORGIO,期刊:SYNLETT, 页码:281-296 , 文章类型: Article,,卷期:2013年-3]
  • Diastereoselective S(N)1-type reactions have been known for many years and have been used in the synthesis of many natural products. It has recently been shown that chiral nucleophiles, obtained using organocatalytic met...
  • Cluster Preface: Process Chemistry
    [作者:YASUDA NOBUYOSHI,期刊:SYNLETT, 页码:298-300 , 文章类型: Article,,卷期:2013年-3]
  • The goal of process chemistry is to identify cost-effective, robust and environmentally friendly manufacturing routes for drug candidates. This article outlines the importance of scientific innovation to overcome the man...
  • Development of a Scalable Synthesis of a VEGFR Inhibitor
    [作者:CHEN YING; CROCKETT RICHARD D; WANG XIN; LARSEN ROBERT D; CUI SHENG; FAUL MARGARET M,期刊:SYNLETT, 页码:301-304 , 文章类型: Article,,卷期:2013年-3]
  • Process development and salt selection for a novel VEGFR inhibitor are described. The overall convergent synthesis involved coupling of three key fragments, 2-chloronicotinoyl chloride, 4-isopropyl-3-methylaniline and 7-...
  • Evolution of the Process for the Preparation of a Selective ErbB VEGF Receptor Inhibitor
    [作者:MUDRYK BOGUSLAW; JOSHI AMIT; ORTIZ ADRIAN; YOUNG IAN S; SAWYER JAMES R; ZHENG BIN; SUGIYAMA MASANO; SHI ZHONGPING; MUESLEHIDDINOGLU JALE; CORBETT R MICHAEL; KRONENTHAL DAVID R; CONLON DAVID A,期刊:SYNLETT, 页码:305-312 , 文章类型: Article,,卷期:2013年-3]
  • An efficient synthetic route to the potent and selective ErbB VEGF receptor inhibitor, BMS-690514 (1) is described. Strategic modifications in both approach and procedure addressed several issues, which led to a safe, ef...
  • Process Development of Halaven (R): Synthesis of the C14-C35 Fragment via Iterative Nozaki-Hiyama-Kishi Reaction-Williamson Ether Cyclization
    [作者:AUSTAD BRIAN C; BENAYOUD FARID; CALKINS TREVOR L; CAMPAGNA SILVIO; CHASE CHARLES E; CHOI HYEONGWOOK; CHRIST WILLIAM; COSTANZO ROBERT; CUTTER JAMES; ENDO ATSUSHI; FANG FRANCIS G; HU YONGBO; LEWIS BRYAN M; LEWIS MICHAEL D; MCKENNA SHAWN; NOLAND THOMAS A; ORR JOHN D; PESANT MARC; SCHNADERBECK MATTHEW J; WILKIE GORDON D; ABE TAICHI; ASAI NAOKI; ASAI YUMI; KAYANO AKIO; KIMOTO YUICHI; KOMATSU YUKI; KUBOTA MANABU; KURODA HIROFUMI; MIZUNO MASANORI; NAKAMURA TAIJU; OMAE TAKAO; OZEKI NAOKI; SUZUKI TAEKO; TAKIGAWA TEIJI; WATANABE TOMOHIRO; YOSHIZAWAB KAZUHIRO,期刊:SYNLETT, 页码:327-332 , 文章类型: Article,,卷期:2013年-3]
  • Multikilogram manufacturing process of the Halaven (R) C14-C35 fragment is described. The synthesis features convergent assembly of subunits by iterative asymmetric Ni/Cr-mediated coupling executed in fixed equipment.
  • Commercial Manufacture of Halaven (R): Chemoselective Transformations En Route to Structurally Complex Macrocyclic Ketones
    [作者:AUSTAD BRIAN C; CALKINS TREVOR L; CHASE CHARLES E; FANG FRANCIS G; HORSTMANN THOMAS E; HU YONGBO; LEWIS BRYAN M; NIU XIANG; NOLAND THOMAS A; ORR JOHN D; SCHNADERBECK MATTHEW J; ZHANG HUIMING; ASAKAWA NAOKI; ASAI NAOKI; CHIBA HIROYUKI; HASEBE TAKASHI; HOSHINO YORIHISA; ISHIZUKA HIROYUKI; KAJIMA TAKASHI; KAYANO AKIO; KOMATSU YUKI; KUBOTA MANABU; KURODA HIROFUMI; MIYAZAWA MAMORU; TAGAMI KATSUYA; WATANABEB TOMOHIRO,期刊:SYNLETT, 页码:333-337 , 文章类型: Article,,卷期:2013年-3]
  • The evolution of the synthesis of Halaven (R) (E7389, INN eribulin mesylate) from a medicinal chemistry process to the execution of the final process on pilot scale is described. The completion of the synthesis of Halave...
  • Palladium-Catalyzed Hydroarylation of Diazoacetic Ester
    [作者:TITANYUK IGOR D; BELETSKAYA IRINA P,期刊:SYNLETT, 页码:355-358 , 文章类型: Article,,卷期:2013年-3]
  • The novel procedure for the Pd-catalyzed hydroarylation of alpha-diazoacetic ester is reported. In the presence of a catalytic amount of PdCl2(PPh3)(2) the three-component reaction of aryl iodides, ethyl diazoacetate, an...