- 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...
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