专利号:US-5606076-A 优先权日:1995-06-07 标 题 :Process for the synthesis of benzo[b]thiophenes 发明人:AIKINS JAMES A; ZHANG TONY Y 权利人:LILLY CO ELI 摘要:The present invention is directed to a process for the synthesis of 2-arylbenzo[b]thiophenes.
专利号:US-5569772-A 优先权日:1995-06-07 标 题:Process for the synthesis of benzo[b]thiophenes 发明人:HOARD DAVID W; LUKE WAYNE D 权利人:LILLY CO ELI 摘要:The present invention is directed to a new process for the synthesis of 2-aryl benzo[b]thiophenes, and to novel intermediates therefor.
专利号:US-5606075-A 优先权日:1995-06-07 标 题:Process for the synthesis of benzo[b]thiophenes 发明人:HOARD DAVID W; LUKE WAYNE D 权利人:LILLY CO ELI 摘要:The present invention is directed to new processes for the synthesis of 2-aryl benzo[b]thiophenes.
专利号:US-7579487-B2 优先权日:2004-05-11 标 题 :Process for making N-sulfonated-amino acid derivatives 发明人:DREHER SPENCER D; IKEMOTO NORIHIRO; SHULTZ C SCOTT; WILLIAMS J MICHAEL 权利人:MERCK & CO INC 摘要:This invention relates to a process for preparing optically active α-amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.
专利号:US-6472539-B1 优先权日:2000-01-07 标题 :Production process of diphosphine oxide and diphosphonate 发明人:YOKOZAWA TOHRU; SAITO TAKAO; SAYO NOBORU; ISHIZAKI TAKERO 权利人:TAKASAGO PERFUMERY CO LTD 摘要:A process for producing a diphosphine oxide or diphosphonate represented by formula (1) as defined, which comprises treating, with a base, a phosphine compound represented by formula (2) as defined and adding the thus-treated phosphine compound to a nonpolar solvent having an oxidative metal compound suspended therein so as to effect dimerization. The present invention makes it possible to produce, conveniently, in a high yield and safely, a diphosphine oxide or diphosphonate which is an intermediate for producing a diphosphine compound useful as a ligand of a metal complex serving as a catalyst for asymmetric synthesis reaction.
专利号:US-5502183-A 优先权日:1992-01-28 标 题 :Steroid intermediates and processes for their preparation 发明人:ANDREWS DAVID R; SUDHAKAR ANANTHA R 权利人:SCHERING CORP 摘要:PCT No. PCT/US93/00211 Sec. 371 Date Jul. 25, 1994 Sec. 102(e) Date Jul. 25, 1994 PCT Filed Jan. 26, 1993 PCT Pub. No. WO93/15103 PCT Pub. Date Aug. 5, 1993.Novel steroids having a 9 alpha -hydroxy or a 9 alpha -carbonate substituent can be prepared from 9 alpha -hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9 alpha -carbonates are prepared by reaction of the corresponding 9 alpha -hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9 alpha -Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17 alpha -ethynyl-17 beta -hydroxy-9 alpha -carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17 alpha -hydroxy 21-ester 9 alpha -carbonate. Elimination of the 9 alpha -carbonate group affords the a 17 alpha -hydroxy, 9(11)ene, which in a few subsequent steps can be converted to a variety of commercially important corticosteroids. Novel 9 alpha -carbonate compounds are prepared in the various reaction steps.