专利号:US-6576777-B2 优先权日:1996-10-18 标 题:Semi-synthesis of a protected baccatin III compound 发明人:ZAMIR LOLITA; CARON GAETAN 权利人:INST NAT RECH SCIENT 摘要:The present invention relates to a semi-synthetic process to convert a naturally occurring taxane into a suitable starting material for the synthesis of paclitaxel and related compounds. Specifically, the present invention relates to a process for the conversion of 9-dihydro-13-acetylbaccatin III into a 7-protected baccatin III which can then be used as starting material for the synthesis of taxane derivatives such as paclitaxel, docetaxel, cephalomannine and other taxanes structurally related to baccatin III. The method as described uses a preparative scale technique which is amenable to commercial scale-up.
专利号:US-7786156-B2 优先权日:2004-01-28 标 题 :Synthesis methods and intermediates for the manufacture of Rizatriptan 发明人:MARTIN PIERRE; BERENS ULRICH; BOUDIER ANDREAS; DOSENBACH OLIVER 权利人:RATIOPHARM GMBH 摘要:The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], n nor a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B]n n nwherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent.n n In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
专利号:US-5637775-A 优先权日:1994-04-28 标 题 :Process for the preparation of halogenated ethers 发明人:GALLEGRA PASQUALE; DEGISCHER GERHARD 权利人:SCHWEIZERHALL SAEUREFAB 摘要:The invention relates to a process for the preparation of compounds of formula I (I) wherein R is mono- or disubstituted lower alkyl, the substituents being selected from halogen and lower alkoxy, with the proviso that said substituents are not present at the carbon atom of the lower alkyl radical R linking the group R to the remainder of the molecule of formula I; R1 is hydrogen, lower alkyl, phenyl or phenyl-lower alkyl; and X is chloro or bromo; which comprises reacting an acetal of formula II, (II) wherein R and R1 are as defined above, with at least one compound of formula R2-X, wherein R2 is hydrogen or X-SO, in which last mentioned case the reaction mixture must contain a catalytically effective amount of N,N-di-lower alkyl-lower alkanoylamide(s) and wherein X is as defined with respect to the compounds of formula I. The compounds of formula I are useful intermediates, suitably for the synthesis of pharmaceutical or fungicidal compounds.
专利号:US-8133999-B2 优先权日:2003-07-30 标题 :Process for preparation of 6, 7-bis(2-methoxyethoxy) quinazolin-4-one 发明人:NISHINO SHIGEYOSHI; HIROTSU KENJI; SHIMA HIDETAKA; ODA HIROYUKI; SUZUKI SHINOBU 权利人:NISHINO SHIGEYOSHI; HIROTSU KENJI; SHIMA HIDETAKA; ODA HIROYUKI; SUZUKI SHINOBU; UBE INDUSTRIES 摘要:6,7-Bis(2-methoxyethoxy)quinazolin-4-one of formula (5) useful in synthesis of an anti-cancer drug can be prepared by a reaction of ethyl 2-amino-4,5-bis(2-methoxyethoxy)benzoate of formula (4) with an orthoformic acid in the presence of an ammonium acetate:
专利号:US-6072062-A 优先权日:1991-07-05 标 题 :Synthesis of C18 -modified vitamin D compounds and compounds resulting therefrom 发明人:VALLES MARIA J; MASCARENAS JOSEL; MOURINO ANTONIO; HALKES SEBASTIANUS J; ZORGDRAGER JAN 权利人:DUPHAR INT RES 摘要:The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group. The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate. The vitamin D compound is of the general formula ##STR1##
专利号:US-5719213-A 优先权日:1993-08-18 标题 :Auxiliary agent for processing plastics, a method for preparing the agent and a method for producing unsaturated polyester resins characterized by supressed vaporization of the monomer component 发明人:KICKO-WALCZAK EWA; GRZYWA EDWARD; WOJDAK WOJCIECH; JAKUBAS TADEUSZ; SZCZEPANOWSKA MARIA; MENTAL ZDZISLAW; KRAWCZYK BARBARA 权利人:INST CHEMII PRZEMYSLOWEI 摘要:The present invention relates to an auxiliary agent for use in the synthesis of unsaturated polyester resins comprising a compound of the general formula n n BCOO--A--COOB' n n and at least one compound selected from the group consisting of fatty acid amides, fatty acid divalent metal salts and their mixtures, whereby styrene emissions from unsaturated polyester resins are suppressed.
摘要:KOPFLER FC ET AL; HUMAN EXPOSURE TO WATER POLLUTANTS; PREPR PAP NATL MEET DIV ENVIRON CHEM AM CHEM SOC 15(1) 185-7 (1975) 摘要:Weast, R.C. (ed.). Handbook of Chemistry and Physics. 57th ed. Cleveland: CRC Press Inc., 1976., p. C-302 摘要:SHACKELFORD WM, KEITH LH; FREQUENCY OF ORG COMPDS IDENTIFIED IN WATER; EPA-600/4-76-062 USEPA ATHENS GA 626 PAGES (1976) 摘要:Ohno, H.; Tomioka, K., Science of Synthesis, (2008) 44, 71.