专利号:US-8110691-B2 优先权日:2006-06-14 标题 :Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process 发明人:DANCSI LAJOSNE; VISKY GYOERGY; TUBA ZOLTAN; CSOERGEI JANOS; MOLNAR CSABA; MAGYARI ENDRENE 权利人:DANCSI LAJOSNE; VISKY GYOERGY; TUBA ZOLTAN; CSOERGEI JANOS; MOLNAR CSABA; MAGYARI ENDRENE; RICHTER GEDEON NYRT 摘要:A new industrial process for the synthesis of solvate-free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.
专利号:US-8183402-B2 优先权日:2007-06-27 标 题:Industrial method for the synthesis of 17-acetoxy-11β[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process 发明人:BODI JOZSEF; VISKY GYOERGY; SZELES JANOS; MAHO SANDOR; SANTA CSABA; CSOERGEI JANOS; TUBA ZOLTAN; TERDY LASZLO; MOLNAR CSABA; ARANYI ANTAL; HORVATH ZOLTAN; BALOGH GABOR 权利人:BODI JOZSEF; VISKY GYOERGY; SZELES JANOS; MAHO SANDOR; SANTA CSABA; CSOERGEI JANOS; TUBA ZOLTAN; TERDY LASZLO; MOLNAR CSABA; ARANYI ANTAL; HORVATH ZOLTAN; BALOGH GABOR; RICHTER GEDEON NYRT 摘要:The present invention relates to a process for the synthesis of the 17-acetoxy-11β-[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (I): n nfrom 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II):
专利号:US-4985567-A 优先权日:1988-03-07 标题:Chiral phosphinopyrrolidine compounds and their use for asymmetric synthesis of optically active compounds 发明人:ACHIWA KAZUO; TAKEDA HIDEO 权利人:KAZUO ACHIWA; FUJI YAKUHIN KOGYO KK 摘要:New chiral phosphinopyrrolidine compounds of the general formula: ##STR1## wherein R 1 is hydrogen or --COA 1 , --COOA 2 , --CONHA 3 , --SO 2 A 4 or --PO(A 5 ) 2 , A 1 , A 2 , A 3 , A 4 and A 5 each represents independently alkyl or aryl, R 2 is phenyl, di(lower-alkyl)aminophenyl, lower-alkoxyphenyl or 3,5-dimethyl-4-methoxyphenyl, and R 3 is phenyl, lower-alkylphenyl, di(lower-alkyl)aminophenyl, lower-alkoxyphenyl or 3,5-dimethyl-4-methoxyphenyl, with the proviso that R 2 and R 3 may not simultaneously by phenyl, p-di(lower-alkyl)-aminophenyl or p-lower-alkoxyphenyl, as well as the use of these compounds as ligand for a metal complex catalyst for asymmetric synthesis of optically active compounds. The new chiral phosphinopyrrolidine compounds are useful ligands which attain both of high optical yield and high reaction efficiency in catalytic asymmetric reduction.
专利号:US-7820831-B2 优先权日:2002-09-11 标 题:Compounds comprising a thiocarbonyl-sulfanyl group which can be used for the radical synthesis of α-perfluoroalkylamine compounds 发明人:ZARD SAMIR; GAGOSZ FABIEN; TOURNIER LUCIE 权利人:CENTRE NAT RECH SCIENT 摘要:The invention relates to compounds having the general formula (I), the method of preparation thereof and the use thereof in organic radical synthesis. The invention also relates to compounds having the formula (II), the method of preparation thereof and a method for preparing compounds having the formula (VIII).
专利号:EP-0447014-B1 优先权日:1990-03-15 标题 :Process for the preparation of intermediates used in the synthesis of progesterone antagonists (synthesis of onapristone) 发明人:OTTOW ECKARD DR; NEEF GUENTER DR; ROHDE RALPH DR 权利人:SCHERING AG 摘要:A process for the preparation of intermediates of the general formula III in which Z, R<1> and R<2> have the meaning indicated in the description, is described and entails a compound of the general formula II in which R<2> and Z have the meaning indicated in formula III, being reacted with a compound of the formula (Hal = halogen) with the addition of a Cu(I) salt. These intermediates are suitable for the preparation of antigestagens (especially Onapristone, EP-A 0 129 499).
专利号:US-8168556-B2 优先权日:2007-10-25 标 题 :Racemoselective synthesis of ansa-metallocene compounds, ansa-metallocene compounds, catalysts comprising them, process for producing an olefin polymer by use of the catalysts, and olefin homo- and copolymers 发明人:SCHULTE JOERG; SELL THORSTEN; THORN MATTHEW GRANT; WINTER ANDREAS; DIMESKA ANITA 权利人:SCHULTE JOERG; SELL THORSTEN; THORN MATTHEW GRANT; WINTER ANDREAS; DIMESKA ANITA; LUMMUS NOVOLEN TECHNOLOGY GMBH 摘要:A metallocene compound with the 4- and 7-positions on the indenyl moiety possessing large aromatic substituents is prepared in accordance with a method which produces substantially 100 percent racemic isomer. Advantageously, polymerization catalysts including the metallocene of the invention provide superior olefin polymerization results.
[参考文献]: Jisheng Zhang, Et Al. Redox Inactive Metal Ion Triggered N-Dealkylation By An Iron Catalyst With Dioxygen Activation: A Lesson From Lipoxygenases. Dalton Trans. 2015 Jun 7;44(21):9847-59.
合成参考文献
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