专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-5087703-A 优先权日:1988-01-28 标题 :Process for synthesis of FK-506 intermediates 发明人:VOLANTE RALPH P; ASKIN DAVID; SHINKAI ICHIRO; RYAN KENNETH M 权利人:MERCK & CO INC 摘要:A process is described for the synthesis of diastereomeric 2-methyl-4-hydroxy-5-protected-hydroxy-hept-6-en-prolinolamides, which are useful as intermediates in the synthesis of the C10-C18 chain of the macrolide structure for the immunosuppressant FK-506. These compounds are also useful as intermediates for preparing lactone ultraviolet radiation absorbers.
专利号:US-5153337-A 优先权日:1991-05-10 标题 :Stereo and enantioselective synthesis of tetrahydro-5-substituted-3-methylene-2-furanmethanols 发明人:RAIFELD YURI E 权利人:AMERICAN CYANAMID CO 摘要:Novel processes and intermediates for the preparation of tetrahydro-5-hydroxy-3-methylene-2-furan-methanol and of tetrahydro-5-[lower alkoxy (C 1 -C 3 )]-3-methylene-2-furanmethanol useful as intermediates in the synthesis of various modified nucleosides having antiviral and other biological activity.
专利号:US-5296620-A 优先权日:1991-05-10 标题:Intermediates in the asymmetric synthesis of 3-substituted furanoside compounds 发明人:RAIFELD YURI E 权利人:AMERICAN CYANAMID CO 摘要:Novel processes, intermediates and reagents for the preparation of 3-substituted furanose or furanoside compounds of Formula I: ##STR1## wherein M is hydrogen or alkyl (C 1 -C 3 ), A is halogen or A may be selected from a moiety of the formula: OR, SR, N 3 , SCR, OC--R or CN wherein R is hydrogen, branched or unbranched alkyl (C 1 -C 4 ) or phenyl which compounds have antiviral and other biological activity.
专利号:WO-2011161690-A1 优先权日:2010-06-23 标题:Processes for the preparation of (+)-n,n-dimethyl-2-[1-(naphthalenyloxy) ethyl] benzene methanamine and intermediates thereof 发明人:MOHAN RAO DODDA; KRISHNA REDDY PINGILI; JITHENDER AADEPU; VENUGOPAL BINGI 权利人:SYMED LABS LTD; MOHAN RAO DODDA; KRISHNA REDDY PINGILI; JITHENDER AADEPU; VENUGOPAL BINGI 摘要:The present invention relates to processes for the preparation of S(+)-N,N-dimethyl-2-[1-(naphthalenyloxy)ethyl]benzene methanamine and intermediates thereof. More particularly the present invention relates to preparation of the compound 3(S)-(+)-N,N-dimethylamino-3-phenyl propanol useful as intermediate in the synthesis of pharmaceutically active compounds.
专利号:US-7812193-B2 优先权日:2003-09-19 标题:Process for enantioselective synthesis of single enantiomers of modafinil by asymmetric oxidation 发明人:REBIERE FRANCOIS; DURET GERARD; PRAT LAURENCE 权利人:CEPHALON FRANCE 摘要:The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of:n a) contacting a pro-chiral sulphide of formula (II) with a metal chiral complex, a base and an oxidizing agent in an organic solvent; and optionally b) isolating the obtained sulphoxide of formula (I); nn nwherein n, Y, R 1 , R 1a , R 2 and R 2a are as defined herein.