专利号:US-6340751-B1 优先权日:1998-07-24 标 题 :Process for the preparation of 4-substituted azetidinone derivatives 发明人:SAITO TAKAO; MURAYAMA TOSHIYUKI; MATSUMOTO TAKAJI; MIURA TAKASHI 权利人:TAKASAGO PERFUMERY CO LTD 摘要:Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): n and (IV): n represented by the following formula (III): n n n MgR 5 R 6   (III) n n n wherein R 5 represents a C 1-12 alkyl group, a C 2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C 1-4 alkyl group, a phenyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom, and R 6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR 7 group (R 7 representing a lower C 1-4 alkyl group, a substituted or unsubstituted phenyl group or a substituted or unsubstituted benzyl group). The process provides an industrially excellent process for the preparation of a 4-substituted azetidinone derivative which permits the selective preparation of an intermediate for the synthesis of a carbapenem antibacterial agent having a desired 1-β′ configuration.
专利号:US-12172982-B2 优先权日:2020-08-12 标 题:Synthesis of quinazoline compounds 发明人:LIM NGIAP-KIE; SHEN JEFF; SIROIS LAUREN ELIZABETH; TIMMERMAN JACOB C; TRACHSEL ETIENNE; WHITE NICHOLAS ANDREW; XU JIE; ZHANG HAIMING; BACHMANN STEPHAN; BIGLER RAPHAEL; CLAGG KYLE BRADLEY PASCUAL; DIPASQUALE ANTONIO GIOVANNI; GOSSELIN FRANCIS; ORCEL UGO JONATHAN; MEIER ROLAND CHRISTOPH 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.
专利号:US-12071422-B2 优先权日:2022-02-07 标 题 :Process for synthesis of quinazoline compounds 发明人:LEBL RENE; LIM NGIAP KIE; MEIER ROLAND CHRISTOPH; ORCEL UGO JONATHAN; SEDELMEIER JOERG; SHEN JEFF; SIROIS LAUREN ELIZABETH; TIMMERMAN JACOB C; TRACHSEL ETIENNE; WHITE NICHOLAS ANDREW; XU JIE; ZHANG HAIMING; BACHMANN STEPHAN; BASS THOMAS MICHAEL; BIGLER RAPHAEL; BURKHARD JOHANNES ADRIAN; CLAGG KYLE BRADLEY PASCUAL; GOSSELIN FRANCIS; HAN CHONG; KALDRE DAINIS; KELLY SEAN M; HEROLD SEBASTIAN; LEITNER CHRISTIAN 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are methods to synthesize compounds useful in the treatment of cancer where such compounds comprise a quinazolinyl core moiety and at least one stereoisomeric or atropisomeric moiety.
专利号:US-2010047841-A1 优先权日:2007-02-27 标 题 :Synthesis of desacetoxytubulysin h and analogs thereof 发明人:WIPF PETER; WANG ZHIYONG 权利人:UNIV PITTSBURGH 摘要:Compounds of formula I, XVI and XXI possess potent cell growth inhibitory activity. These compounds are described have therapeutic utility, particularly in the treatment of cancer as well as conditions and disorders related to uncontrolled cell growth: n n n n n n n n n n wherein the variables R 1 , R 2 , R 3 , R 4 , R 5 , X, Y and Z are described herein.
专利号:US-2023416243-A1 优先权日:2020-11-06 标 题 :Process for Preparing Heterocyclic Methanone Compounds and AZA-Bicyclo Intermediates Thereof 发明人:GRUGEL CHRISTIAN 权利人:ACTINOGEN MEDICAL LTD 摘要:The present disclosure relates to a process for synthesis of heterocyclic methanone compounds, and in particular 3′-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds, and aza-bicyclo intermediates thereof. In particular, the present disclosure also relates to a process for the synthesis of Xanamem. The present disclosure also relates to a process for the synthesis of optionally protected aza-bicyclo intermediate compounds. The present disclosure also relates to 3′-substituted, 3-hydroxyl-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1h-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds and aza-bicyclo intermediate compounds thereof.
专利号:US-8207337-B2 优先权日:2007-01-29 标 题:Reagent for organic synthesis reaction containing organic triol borate salt 发明人:MIYAURA NORIO; YAMAMOTO YASUNORI 权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD 摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).