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31. 发明公开

EP0253838A4 CATALYTIC METHOD FOR PRODUCING FLUOROAROMATIC COMPOUNDS USING N-SEC-ALKYL PYRIDINIUM SALTS. 失效转让
标题翻译： KATALYTISCHES VERFAHREN ZUR HERSTELLUNG VON FLUORAOMATISCHEN VERBINDUNGEN MITTELS N-SEK-ALKYLPYRIDINIUMSALZE。
公开(公告)号：EP0253838A4
公开(公告)日：1988-07-04
申请号：EP87900618
申请日：1986-12-30
申请人： MALLINCKRODT INC
发明人： CANTRELL GARY L
IPC分类号： C07B61/00 , B01J31/02 , C07B31/00 , C07B39/00 , C07C67/00 , C07C201/00 , C07C205/07 , C07C205/12 , C07D213/00 , C07D213/74
CPC分类号： C07D213/74
摘要： N-secondary-alkyldiorganoaminopyridinium salts which are useful as phase transfer catalysts for facilitating preparation of fluoroaromatic compounds (such as fluoronitrobenzene compounds) from the corresponding chloroaromatic compounds (such as chloronitrobenzene compounds).
摘要翻译： N-仲烷基二有机氨基吡啶鎓盐，其可用作相转移催化剂以便于从相应的氯代芳族化合物（例如氯硝基苯化合物）制备氟代芳族化合物（例如氟代硝基苯化合物）。

32. 发明专利

CA2674099C PREPARATION OF AMIDES FROM AN ACID AND AMINE FOR INTERMEDIATES IN THE SYNTHESIS OF MORPHINANS 未知
公开(公告)号：CA2674099C
公开(公告)日：2016-03-22
申请号：CA2674099
申请日：2007-12-10
申请人： MALLINCKRODT INC
发明人： GROTE CHRISTOPHER W , WANG PETER X , MOSER FRANK W , CANTRELL GARY L
IPC分类号： C07C235/34 , C07C231/02 , C07C303/30 , C07C309/66
摘要： The present invention is directed to processes for the synthesis of morphinans, in particular, those of Formula 502: (see formula 502) In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCI3 that is necessary to form the 3,4-dihydroisoquinoline.

33. 发明专利

CA2672745C A PROCESS FOR THE PREPARATION OF HEXAHYDROISOQUINOLINES FROM 1,2,3,4-TETRAHYDROISOQUINOLINES 未知
公开(公告)号：CA2672745C
公开(公告)日：2016-03-22
申请号：CA2672745
申请日：2007-12-10
申请人： MALLINCKRODT INC
发明人： WANG PETER X , CANTRELL GARY L , MAGPARANGALAN DAN P , MOSER FRANK W , BAO JIAN , GROTE CHRISTOPHER W
IPC分类号： C07D217/20
摘要： The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4- dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.

34. 发明专利

CA2709862C SINOMENINE DERIVATIVES AND PROCESSES FOR THEIR SYNTHESIS 未知
公开(公告)号：CA2709862C
公开(公告)日：2016-03-15
申请号：CA2709862
申请日：2008-12-17
申请人： MALLINCKRODT INC
发明人： WANG PETER X , JIANG TAO , CANTRELL GARY L , BERBERICH DAVID W , TRAWICK BOBBY N , LIAO SUBO , BRANDT JOHN
IPC分类号： C07D221/28 , A61K31/485 , C07D489/02
摘要： The invention generally provides processes and intermediate compounds useful for the production of sinomenine derivatives. In particular, the process may encompass synthetic routes for the production of (+)-sinomenine derivatives and their intermediates.

35. 发明专利

CA2610859C A SYNTHETIC ROUTE TO 14-HYDROXYL OPIATES THROUGH 1-HALO-THEBAINE OR ANALOGS 未知
公开(公告)号：CA2610859C
公开(公告)日：2013-11-12
申请号：CA2610859
申请日：2006-05-22
申请人： MALLINCKRODT INC
发明人： WANG PETER XIANQI , MOSER FRANK W , CANTRELL GARY L , MAGPARANGALAN DANIEL P , BAO JIAN
IPC分类号： C07D489/08 , C07D489/00
摘要： Novel methods of synthesis of known and novel 14-hydroxyl optiates as depicted in Formula 17, through 1-halothebaine and derivatives thereof are described. (see formula 17)

36. 发明专利

ES2369821T3 DISPOSITIVOS MEDICOS PARA ADMINISTRACION LOCALIZADA DE MEDICAMENTO. 未知
公开(公告)号：ES2369821T3
公开(公告)日：2011-12-07
申请号：ES09012859
申请日：2007-11-15
申请人： MALLINCKRODT INC
发明人： CANTRELL GARY L , BERBERICH DAVID W
IPC分类号： A61F2/88 , A61F2/90
摘要： Un dispositivo (10) para administrar un agente activo (18) a un sujeto, incluyendo el dispositivo (10): un elemento alargado (12) que tiene una cavidad interna (14) definida en él, teniendo además el elemento alargado (12) un agujero (16) que se extiende desde la cavidad interna (14) al exterior del elemento alargado (12), donde dicho agujero (16) tiene un tamaño suficiente para evitar que glóbulos sanguíneos entren en la cavidad interna (14); y una estructura polimérica (20) dispuesta en la cavidad interna (14), caracterizado porque la estructura polimérica (20) tiene una pluralidad de primeros lugares receptores simulados (22), configurado cada uno para unir un primer agente activo (18), donde cada primer lugar receptor simulado (22) incluye un lugar receptor simulado artificial, y donde cada primer lugar receptor simulado se define en la estructura polimérica (20) por una impresión molecular de dicho primer agente activo (18).

37. 发明专利

AT518504T 未知
公开(公告)号：AT518504T
公开(公告)日：2011-08-15
申请号：AT09012859
申请日：2007-11-15
申请人： MALLINCKRODT INC
发明人： CANTRELL GARY L , BERBERICH DAVID W
IPC分类号： A61F2/88 , A61F2/90

38. 发明专利

AT517869T 未知
公开(公告)号：AT517869T
公开(公告)日：2011-08-15
申请号：AT07837847
申请日：2007-09-06
申请人： MALLINCKRODT INC
发明人： WANG PETER XIANQI , MOSER FRANK W , CANTRELL GARY L , GROTE CHRISTOPHER W
IPC分类号： C07D217/20
摘要： The present invention is directed to processes for the synthesis of morphinan-6-ones and salts, intermediates, and analogs thereof.

39. 发明专利

NZ579469A PROCESS FOR THE PREPARATION OF QUATERNARY N-ALKYL MORPHINAN ALKALOID SALTS 未知
公开(公告)号：NZ579469A
公开(公告)日：2011-02-25
申请号：NZ57946908
申请日：2008-03-06
申请人： MALLINCKRODT INC
发明人： WANG PETER X , CANTRELL GARY L , HALVACHS ROBERT E , ROESCH KEVIN R , BUEHLER HENRY J , HAAR JOSEPH P
IPC分类号： C07D489/02 , C07D489/04 , C07D489/08
摘要： Disclosed is a process for the preparation of a quaternary derivative of a tertiary N-substituted morphinan alkaloid having a C(3) hydroxy substituent, the process comprising (i) combining a tertiary N-substituted morphinan alkaloid substrate with an alkylating agent in an anhydrous solvent system to form a reaction product mixture containing the quaternary derivative of the tertiary N-substituted morphinan alkaloid substrate and any unreacted tertiary N-substituted morphinan alkaloid substrate, the solvent system comprising an anhydrous aprotic dipolar solvent with the aprotic dipolar solvent constituting at least 25 wt.% of the solvent system, and (ii) adding an anhydrous acid to the reaction product mixture to suppress ionization of the C(3) hydroxy substituent and production of C(3) alkoxy side products. Also disclosed is a process for the preparation of a quaternary derivative of a tertiary N-substituted morphinan alkaloid, the process comprising: (i) adding less than 3 equivalents of a solution of an alkylating agent dissolved in an anhydrous dipolar aprotic solvent to a tertiary N-substituted morphinan alkaloid substrate dissolved in an anhydrous solvent system, to form a reaction product mixture containing the quaternary derivative of the tertiary N-substituted morphinan alkaloid substrate and any unreacted tertiary N-substituted morphinan alkaloid substrate, the rate of addition of the alkylating agent being less than 0.02 equivalents of alkylating agent per equivalent of substrate per minute based upon the concentration of substrate in the reaction mixture; wherein the solution of the alkylating agent is maintained at a temperature below about 0 deg C and is added to the reaction mixture at a temperature of between about 50 deg C and about 85 deg C so as to inhibit O-alkylation at the C(3) hydroxide to less than 10% and inhibit evaporative loss of alkylating agent; and, (ii) adding an anhydrous acid to the reaction mixture to enhance product formation and inhibit side products when the substrate contains a C(3) hydroxy substituent.

40. 发明专利

DE602006019246D1 SYNTHETISCHE ROUTE ZU 14-HYDROXYLOPIATEN ÜBER 1-HALOGENTHEBAIN ODER ANALOGA 未知
公开(公告)号：DE602006019246D1
公开(公告)日：2011-02-10
申请号：DE602006019246
申请日：2006-05-22
申请人： MALLINCKRODT INC
发明人： WANG PETER XIANQI , MOSER FRANK W , CANTRELL GARY L , MAGPARANGALAN DANIEL P , BAO JIAN
IPC分类号： C07D489/08 , C07D489/00

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